HY-10211-1ml | Tanespimycin [75747-14-7] Biotrend USA

Description

Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC₅₀ of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90^[1]^[5]. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression^[3].

IC₅₀ & Target^[5]

HSP90

5 nM (IC₅₀)

Autophagy

Mitophagy

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	1287 nM Compound: 2, 17-AAG	Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
A-375	IC₅₀	32 nM Compound: 2, 17-AAG	Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening	[PMID: 19552433]
A-375	IC₅₀	4 nM Compound: 2, 17-AAG	Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening	[PMID: 19552433]
A-431	IC₅₀	0.069 μM Compound: 17-AAG	Cytotoxicity against human A431 cells after 72 hrs Cytotoxicity against human A431 cells after 72 hrs	[PMID: 22538015]
A-431	IC₅₀	0.07 μM Compound: 17-AAG	Antiproliferative activity against human A431 cells after 72 hrs Antiproliferative activity against human A431 cells after 72 hrs	[PMID: 20655237]
A-431	IC₅₀	89 nM Compound: 17-Aag	Cytotoxicity against human A431 cells after 72 hrs by MTT assay Cytotoxicity against human A431 cells after 72 hrs by MTT assay	[PMID: 25277067]
A549	IC₅₀	> 10 μM Compound: 4; 17-AAG	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
A549	IC₅₀	> 10 μM Compound: 17-AAG	Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
A549	GI₅₀	0.0075 μM Compound: III; 17AAG	Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 31655430]
A549	GI₅₀	0.08 μM Compound: 1; 17-AAG	Antiproliferative activity against human A549 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
A549	IC₅₀	0.286 μM Compound: 2; 17-AAG	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 28073608]
A549	IC₅₀	81 nM Compound: 17-Aag	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25277067]
AU565	IC₅₀	0.003 μM Compound: 2, 17-AAG	Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening	[PMID: 19552433]
AU565	IC₅₀	8 nM Compound: 2, 17-AAG	Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening	[PMID: 19552433]
BGC-823	IC₅₀	847 nM Compound: 17-Aag	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 25277067]
BT-474	IC₅₀	0.01 μM Compound: 17-AAG	Antiproliferative activity against human BT474 cells by MTS assay Antiproliferative activity against human BT474 cells by MTS assay	[PMID: 17488003]
BT-474	GI₅₀	5 nM Compound: 3, 17-AAG	Growth inhibition of human BT474 cells assessed as ATP level after 4 days Growth inhibition of human BT474 cells assessed as ATP level after 4 days	[PMID: 19410458]
CNE-2	IC₅₀	3.03 μM Compound: 17-AAG	Cytotoxicity in human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33543615]
CNE2Z	IC₅₀	8.41 μM Compound: 17-AAG	Antiproliferative activity against human CNE2Z cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human CNE2Z cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
DU-145	IC₅₀	0.282 μM Compound: 2; 17-AAG	Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay	[PMID: 28073608]
DU-145	IC₅₀	68.3 μM Compound: 17-AAG	Cytotoxicity against DU145 cells after 72 hrs Cytotoxicity against DU145 cells after 72 hrs	[PMID: 17181154]
ECa-109 cell line	IC₅₀	1.1 μM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human ECA109 cells after 48 hrs by MTT assay Cytotoxicity against human ECA109 cells after 48 hrs by MTT assay	[PMID: 23621840]
GES1	CC₅₀	7.94 μM Compound: 4; 17-AAG	Cytotoxicity against human GES1 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human GES1 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
HCC827	GI₅₀	56 nM Compound: 3, 17-AAG	Growth inhibition of human tarceva and iressa-resistant HCC827 cells assessed as ATP level after 4 days Growth inhibition of human tarceva and iressa-resistant HCC827 cells assessed as ATP level after 4 days	[PMID: 19410458]
HCT-116	GI₅₀	0.16 μM Compound: 1b, 17-AAG	Growth inhibition of human HCT116 cells after 24 hrs by SRB assay Growth inhibition of human HCT116 cells after 24 hrs by SRB assay	[PMID: 18020435]
HCT-116	GI₅₀	0.34 μM Compound: 1; 17-AAG	Antiproliferative activity against human HCT116 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human HCT116 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
HCT-116	GI₅₀	0.34 μM Compound: III; 17AAG	Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 31655430]
HCT-116	IC₅₀	202 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human HCT116 cells after 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs	[PMID: 19231864]
HCT-116	IC₅₀	56.5 nM Compound: 17-AAG	Growth inhibition of human HCT116 cells after 24 hrs by [3H]thymidine uptake assay Growth inhibition of human HCT116 cells after 24 hrs by [3H]thymidine uptake assay	[PMID: 20014866]
HCT-15	IC₅₀	1487 nM Compound: 2, 17-AAG	Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
HeLa	IC₅₀	> 1000 μM Compound: III; 17AAG	Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay	[PMID: 31655430]
HeLa	IC₅₀	0.2 μM Compound: 17-AAG	Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay	[PMID: 27266997]
HeLa	IC₅₀	108.2 μM Compound: 17-AAG	Cytotoxicity against HeLa cells after 72 hrs Cytotoxicity against HeLa cells after 72 hrs	[PMID: 17181154]
HeLa	IC₅₀	128 nM Compound: 17-Aag	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 25277067]
HeLa	IC₅₀	19.4 μM Compound: 17-AAG	Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33543615]
Hep 3B2	GI₅₀	0.08 μM Compound: 1; 17-AAG	Antiproliferative activity against human Hep3B cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human Hep3B cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
HepG2	IC₅₀	0.32 μM Compound: 17-AAG	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
HepG2	IC₅₀	0.33 μM Compound: 4; 17-AAG	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
HepG2	IC₅₀	8 μM Compound: 17-AAG	Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33543615]
HepG2	IC₅₀	91 nM Compound: 17-Aag	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 25277067]
HT-29	IC₅₀	0.1 nM Compound: 2, 17-AAG	Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
HUVEC	GI₅₀	< 0.1 μM Compound: 1; 17-AAG	Antiproliferative activity against human HUVEC cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human HUVEC cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
HUVEC	IC₅₀	282 nM Compound: 17-Aag	Cytotoxicity against HUVEC cells after 72 hrs by MTT assay Cytotoxicity against HUVEC cells after 72 hrs by MTT assay	[PMID: 25277067]
K562	IC₅₀	0.15 μM Compound: 1, 17-AAG	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay	[PMID: 24565573]
K562	IC₅₀	126 nM Compound: 2, 17-AAG	Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
K562	GI₅₀	48 nM Compound: 3, 17-AAG	Growth inhibition of human K562 cells assessed as ATP level after 4 days Growth inhibition of human K562 cells assessed as ATP level after 4 days	[PMID: 19410458]
L02	CC₅₀	11.65 μM Compound: 4; 17-AAG	Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
L02	IC₅₀	99 nM Compound: 17-Aag	Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay	[PMID: 25277067]
LNCaP	IC₅₀	0.16 μM Compound: 17-AAG	Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay	[PMID: 25105924]
LNCaP	IC₅₀	82 nM Compound: 2, 17-AAG	Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
LoVo	IC₅₀	0.26 μM Compound: 4; 17-AAG	Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
MCF7	IC₅₀	0.01 μM Compound: 17-AAG	Antiproliferative activity against human MCF7 cells by MTS assay Antiproliferative activity against human MCF7 cells by MTS assay	[PMID: 17488003]
MCF7	IC₅₀	0.029 μM Compound: 17-AAG	Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay	[PMID: 27153346]
MCF7	IC₅₀	0.09 μM Compound: 1b, 17-AAG	Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 21920765]
MCF7	IC₅₀	0.192 μM Compound: 2; 17-AAG	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 28073608]
MCF7	IC₅₀	0.3 nM Compound: 2, 17-AAG	Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
MCF7	IC₅₀	5 nM Compound: 17-AAG	Antiproliferative activity against human MCF7 cells measured after 5 days by MTS assay Antiproliferative activity against human MCF7 cells measured after 5 days by MTS assay	[PMID: 27153346]
MCF7	IC₅₀	58 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human MCF7 cells after 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs	[PMID: 19231864]
MCF7	IC₅₀	662 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human MCF7 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol Cytotoxicity against human MCF7 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol	[PMID: 19231864]
MDA-MB-231	GI₅₀	0.27 μM Compound: 1; 17-AAG	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
MDA-MB-231	IC₅₀	0.28 μM Compound: 17-Aag	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25277067]
MDA-MB-231	IC₅₀	0.28 μM Compound: 17-AAG	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25105924]
MDA-MB-231	IC₅₀	0.52 μM Compound: 17-AAG	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 27266997]
MDA-MB-231	IC₅₀	1.79 μM Compound: 17-AAG	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
MDA-MB-231	IC₅₀	194 nM Compound: 2, 17-AAG	Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
MDA-MB-468	IC₅₀	1.57 μM Compound: 17-AAG	Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs by MTT assay	[PMID: 27153346]
MDA-MB-468	IC₅₀	1500 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against NQ01-deficient human MDA468 cells after 72 hrs Cytotoxicity against NQ01-deficient human MDA468 cells after 72 hrs	[PMID: 19231864]
MDA-MB-468	GI₅₀	780 nM Compound: 3, 17-AAG	Growth inhibition of human MDA-MB-468 cells assessed as ATP level after 4 days Growth inhibition of human MDA-MB-468 cells assessed as ATP level after 4 days	[PMID: 19410458]
MRC5	CC₅₀	14.24 μM Compound: 4; 17-AAG	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
MV4-11	GI₅₀	11 nM Compound: 3, 17-AAG	Growth inhibition of human MV4-11 cells assessed as ATP level after 4 days Growth inhibition of human MV4-11 cells assessed as ATP level after 4 days	[PMID: 19410458]
NCI-H1299	IC₅₀	0.2 μM Compound: 17-AAG	Antiproliferative activity against human H1299 cells after 48 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against human H1299 cells after 48 hrs by resazurin dye-based fluorescence assay	[PMID: 28426997]
NCI-H1975	GI₅₀	0.16 μM Compound: III; 17AAG	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 31655430]
NCI-H1975	GI₅₀	35 nM Compound: 3, 17-AAG	Growth inhibition of human tarceva and iressa-resistant NCI-H1975 cells assessed as ATP level after 4 days Growth inhibition of human tarceva and iressa-resistant NCI-H1975 cells assessed as ATP level after 4 days	[PMID: 19410458]
NCI-H460	IC₅₀	0.01 μM Compound: 17-AAG	Cytotoxicity against human NCI-H460 cells after 72 hrs Cytotoxicity against human NCI-H460 cells after 72 hrs	[PMID: 22538015]
NCI-H460	IC₅₀	255 nM Compound: 2, 17-AAG	Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
NCI-H596	IC₅₀	1600 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against NQ01-deficient human NCI-H596 cells after 72 hrs Cytotoxicity against NQ01-deficient human NCI-H596 cells after 72 hrs	[PMID: 19231864]
NCI-N87	GI₅₀	1 nM Compound: 3, 17-AAG	Growth inhibition of human NCI-N87 cells assessed as ATP level after 4 days Growth inhibition of human NCI-N87 cells assessed as ATP level after 4 days	[PMID: 19410458]
NCM460	CC₅₀	14.21 μM Compound: 4; 17-AAG	Cytotoxicity against human NCM460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human NCM460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
OVCAR-3	IC₅₀	0.48 μM Compound: 4; 17-AAG	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
PANC-1	IC₅₀	3.21 μM Compound: 4; 17-AAG	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
PC-3	IC₅₀	0.062 μM Compound: 17-AAG	Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
PC-3	IC₅₀	9 nM Compound: 2, 17-AAG	Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
SGC-7901	IC₅₀	> 10 μM Compound: 4; 17-AAG	Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
SK-BR-3	EC₅₀	< 0.1 μM Compound: 1, 17-AAG	Inhibition of Hsp90alpha in human SKBR3 cells assessed as ErbB2 degradation by Western blot analysis Inhibition of Hsp90alpha in human SKBR3 cells assessed as ErbB2 degradation by Western blot analysis	[PMID: 21106457]
SK-BR-3	IC₅₀	0.038 μM Compound: 17-AAG	Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
SK-BR-3	EC₅₀	0.06 μM Compound: 1, 17-AAG	Inhibition of Hsp90alpha in human SKBR3 cells assessed as up-regulation of HSP70 protein by Western blot analysis Inhibition of Hsp90alpha in human SKBR3 cells assessed as up-regulation of HSP70 protein by Western blot analysis	[PMID: 21106457]
SK-BR-3	IC₅₀	27 nM Compound: 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-Glo assay Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-Glo assay	[PMID: 15844961]
SK-BR-3	IC₅₀	33 nM Compound: 1b, 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay	[PMID: 19405528]
SK-BR-3	IC₅₀	410 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol Cytotoxicity against human SKBR3 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol	[PMID: 19231864]
SK-BR-3	IC₅₀	44 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs	[PMID: 19231864]
SK-MEL-5	IC₅₀	134 nM Compound: 2, 17-AAG	Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
SK-OV-3	IC₅₀	0.22 μM Compound: 17-AAG	Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
SK-OV-3	IC₅₀	240 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human SKOV3 cells after 72 hrs Cytotoxicity against human SKOV3 cells after 72 hrs	[PMID: 19231864]
SMMC-7721	IC₅₀	0.19 μM Compound: 17-AAG	Antiproliferative activity against human SMMC7721 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SMMC7721 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
SW480	IC₅₀	0.28 μM Compound: 17-AAG	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
SW480	IC₅₀	572 nM Compound: 17-Aag	Cytotoxicity against human SW480 cells after 72 hrs by MTT assay Cytotoxicity against human SW480 cells after 72 hrs by MTT assay	[PMID: 25277067]
SW-620	IC₅₀	328 nM Compound: 2, 17-AAG	Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
U-87MG ATCC	IC₅₀	> 10 μM Compound: 17-AAG	Antiproliferative activity against human U-87 MG cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human U-87 MG cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]

In Vitro

Tanespimycin causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. Tanespimycin inhibits prostate cancer cell lines with IC₅₀s ranged from 25-45 nM (LNCaP, 25 nM; LAPC-4, 40 nM; DU-145, 45 nM; and PC-3, 25 nM)^[1].
Tanespimycin (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells^[2]. Tanespimycin inhibits cell growth and induces G2/M cell cycle arrest and apoptosis in CCA cells together with the down-regulation of Bcl-2, Survivin and Cyclin B1, and the up-regulation of cleaved PARP^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tanespimycin (25-200 mg/kg, i.p.) causes a dose-dependent decline in AR, HER2, and Akt expression in prostate cancer xenografts. Tanespimycin treatment at doses sufficient to induce AR, HER2, and Akt degradation results in the dose-dependent inhibition of androgen-dependent and -independent prostate cancer xenograft growth without toxicity^[1].
Tanespimycin (60 mg/kg) with Rapamycin (30 mg/kg) inhibits A549 and MDA-MB-231 tumor growth and effects tumor cures in MDA-MB-231 tumor-bearing animals by tail vein injection^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

585.69

Formula

C₃₁H₄₃N₃O₈

CAS No.

75747-14-7

Appearance

Solid

Color

Purple to purplish red

SMILES

O=C(C(NC(/C(C)=C/C=C\[C@H](OC)[C@H](/C(C)=C/[C@@H]([C@H]([C@H](C[C@@H](C1)C)OC)O)C)OC(N)=O)=O)=CC2=O)C1=C2NCC=C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (85.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7074 mL	8.5369 mL	17.0739 mL
5 mM	0.3415 mL	1.7074 mL	3.4148 mL
10 mM	0.1707 mL	0.8537 mL	1.7074 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (8.54 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (8.54 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.62 mg/mL (2.77 mM); Clear solution

This protocol yields a clear solution of ≥ 1.62 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (17.07 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 5 mg/mL (8.54 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.01%

Select Batch:

SDS (393 KB)

COA (252 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Solit DB, et al. 17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts.Clin Cancer Res, 2002, 8(5), 986-993. [Content Brief]

[2]. Raja, Srikumar M., et al. 17-AAG induces enhanced ubiquitinylation and lysosomal pathway-dependent ErbB2 degradation and cytotoxicity in ErbB2-overexpressing breast cancer cells. Cancer Biology & Therapy (2008), 7(10), 163 [Content Brief]

[3]. Zhang J, et al. The heat shock protein 90 inhibitor 17-AAG suppresses growth and induces apoptosis in human cholangiocarcinoma cells.Clin Exp Med. 2012 Sep 7. [Content Brief]

[4]. Newman B, et al. HSP90 Inhibitor 17-AAG Selectively Eradicates Lymphoma Stem Cells.Cancer Res. 2012 Sep 1;72(17):4551-61. Epub 2012 Jun 29. [Content Brief]

[5]. Kamal A, et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors. Nature. 2003 Sep 25;425(6956):407-10. [Content Brief]

[6]. Enomoto A, et al. The HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin modulates radiosensitivity by downregulating serine/threonine kinase 38 via Sp1 inhibition. Eur J Cancer. 2013 Nov;49(16):3547-58. [Content Brief]

Cell Assay ^[1]	For the Alamar Blue proliferation assay, 2-4×10³ cells are plated in 96-well plates. Later (48 h), cells are treated with Tanespimycin for 96 h or 0.01% DMSO as control. On day 4, Alamar Blue viability assay is performed as described elsewhere. IC₅₀ and IC₉₀s are calculated as the doses of Tanespimycin required to inhibit cell growth by 50 and 90%, respectively. Cell cycle distribution is assayed as described previously with a Becton Dickinson fluorescence-activated cell sorter and analyzed by the Cell Cycle Multicycle system. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Tanespimycin is dissolved in an EPL vehicle. To aid in the identification of an optimal dose and schedule, nontumor bearing mice are treated by i.p. injection with 25-200 mg/kg of Tanespimycin 5 days/week for 3 weeks or by the EPL vehicle alone. Serum samples are taken from each group, and equal volumes are pooled on days 5, 10, and 15 of treatment for serum chemistry and liver function analysis. At sacrifice, plasma samples are collected for complete blood count. A gross necropsy is performed on all of the mice, and a complete necropsy, including histopathology, is performed on 1 animal/group. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Solit DB, et al. 17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts.Clin Cancer Res, 2002, 8(5), 986-993. [Content Brief] [2]. Raja, Srikumar M., et al. 17-AAG induces enhanced ubiquitinylation and lysosomal pathway-dependent ErbB2 degradation and cytotoxicity in ErbB2-overexpressing breast cancer cells. Cancer Biology & Therapy (2008), 7(10), 163 [Content Brief] [3]. Zhang J, et al. The heat shock protein 90 inhibitor 17-AAG suppresses growth and induces apoptosis in human cholangiocarcinoma cells.Clin Exp Med. 2012 Sep 7. [Content Brief] [4]. Newman B, et al. HSP90 Inhibitor 17-AAG Selectively Eradicates Lymphoma Stem Cells.Cancer Res. 2012 Sep 1;72(17):4551-61. Epub 2012 Jun 29. [Content Brief] [5]. Kamal A, et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors. Nature. 2003 Sep 25;425(6956):407-10. [Content Brief] [6]. Enomoto A, et al. The HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin modulates radiosensitivity by downregulating serine/threonine kinase 38 via Sp1 inhibition. Eur J Cancer. 2013 Nov;49(16):3547-58. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7074 mL	8.5369 mL	17.0739 mL	42.6847 mL
	5 mM	0.3415 mL	1.7074 mL	3.4148 mL	8.5369 mL
	10 mM	0.1707 mL	0.8537 mL	1.7074 mL	4.2685 mL
	15 mM	0.1138 mL	0.5691 mL	1.1383 mL	2.8456 mL
	20 mM	0.0854 mL	0.4268 mL	0.8537 mL	2.1342 mL
	25 mM	0.0683 mL	0.3415 mL	0.6830 mL	1.7074 mL
	30 mM	0.0569 mL	0.2846 mL	0.5691 mL	1.4228 mL
	40 mM	0.0427 mL	0.2134 mL	0.4268 mL	1.0671 mL
	50 mM	0.0341 mL	0.1707 mL	0.3415 mL	0.8537 mL
	60 mM	0.0285 mL	0.1423 mL	0.2846 mL	0.7114 mL
	80 mM	0.0213 mL	0.1067 mL	0.2134 mL	0.5336 mL

Tanespimycin Related Classifications

Cell Cycle/DNA Damage Metabolic Enzyme/Protease Autophagy Anti-infection Apoptosis
HSP Autophagy Mitophagy Bacterial Apoptosis Antibiotic

Tanespimycin [75747-14-7]

Cat# HY-10211-1ml

Brand : MedChemExpress

Other Forms of Tanespimycin:

View All HSP Isoform Specific Products:

View All Antibiotic Isoform Specific Products:

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tanespimycin Related Classifications

Keywords:

You might also be interested by the following products:

Tanespimycin [75747-14-7]

Cat# HY-10211-1ml

Brand : MedChemExpress

Other Forms of Tanespimycin:

View All HSP Isoform Specific Products:

View All Antibiotic Isoform Specific Products:

Tanespimycin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tanespimycin Related Classifications

Keywords:

You might also be interested by the following products: