Reagents and instruments for immunology, cell biology and molecular biology.

Goat anti-Human IgG Fc, TRITC conjugated

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Cat# AS101197

Size : 1mg

Brand : Agrisera

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Description

Onalespib (AT13387) is a long-acting second-generation Hsp90 inhibitor with a K_d of 0.71 nM.

IC₅₀ & Target^[1]

HSP90

0.71 nM (Kd)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.05 μM Compound: 8; AT13387	Antiproliferative activity against human A549 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
A549	IC₅₀	0.44 μM Compound: AT13387	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30784881]
BT-474	IC₅₀	0.032 μM Compound: 8; AT13387	Antiproliferative activity against human BT-474 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-474 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
GIST430	IC₅₀	34 nM Compound: 8; AT-13387	Cytotoxicity against imatinib-resistant human GIST430 cells assessed as decrease in cell viability after 7 days by alamar blue assay Cytotoxicity against imatinib-resistant human GIST430 cells assessed as decrease in cell viability after 7 days by alamar blue assay	[PMID: 26844689]
GIST48	IC₅₀	55 nM Compound: 8; AT-13387	Cytotoxicity against imatinib-resistant human GIST48 cells assessed as decrease in cell viability after 7 days by alamar blue assay Cytotoxicity against imatinib-resistant human GIST48 cells assessed as decrease in cell viability after 7 days by alamar blue assay	[PMID: 26844689]
HCT-116	IC₅₀	0.07 μM Compound: 8; AT13387	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
HCT-116	IC₅₀	0.08 μM Compound: AT-13387	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 24763261]
HCT-116	IC₅₀	48 nM Compound: 35	Cytotoxicity against human HCT116 cells by Alamar blue assay Cytotoxicity against human HCT116 cells by Alamar blue assay	[PMID: 20662534]
HepG2	IC₅₀	0.018 μM Compound: 8; AT13387	Antiproliferative activity against human HepG2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
K562	IC₅₀	0.038 μM Compound: 8; AT13387	Antiproliferative activity against human K562 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human K562 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
L02	IC₅₀	11.64 μM Compound: 8; AT13387	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
MCF7	IC₅₀	0.02 μM Compound: 8; AT13387	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
MCF7	IC₅₀	0.032 μM Compound: AT13387	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 29028527]
MCF7	IC₅₀	0.28 μM Compound: AT-13387	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: 24763261]
MCF7	IC₅₀	0.29 μM Compound: AT13387	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30784881]
MDA-MB-231	IC₅₀	0.038 μM Compound: 8; AT13387	Antiproliferative activity against human MDA-MB-231 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
MDA-MB-468	IC₅₀	0.066 μM Compound: 8; AT13387	Antiproliferative activity against human MDA-MB-468 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
MKN-28	IC₅₀	0.129 μM Compound: 8; AT13387	Antiproliferative activity against human MKN-28 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MKN-28 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
MV4-11	IC₅₀	0.011 μM Compound: 8; AT13387	Antiproliferative activity against human MV4-11 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
NCI-H1299	IC₅₀	0.37 μM Compound: AT13387	Antiproliferative activity against human NCI-H1299 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells after 72 hrs by MTT assay	[PMID: 30784881]
NCI-H3122	IC₅₀	52 nM Compound: AT13387	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay	[PMID: 29698859]
SK-BR-3	IC₅₀	0.045 μM Compound: AT13387	Antiproliferative activity against human SKBR3 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human SKBR3 cells incubated for 72 hrs by MTT assay	[PMID: 29028527]
SK-BR-3	IC₅₀	0.071 μM Compound: 8; AT13387	Antiproliferative activity against human SK-BR-3 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
SK-BR-3	IC₅₀	0.14 μM Compound: AT-13387	Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay	[PMID: 24763261]
T47D	IC₅₀	0.024 μM Compound: 8; AT13387	Antiproliferative activity against human T47D assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human T47D assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
U2OS	IC₅₀	0.067 μM Compound: 8; AT13387	Antiproliferative activity against human U2OS assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human U2OS assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]

In Vitro

Onalespib (Compound 35) is a potent inhibitor of Hsp90, with K_d of 0.71 nM. Onalespib shows potent antiproliferative activity in HCT116 cells, with an IC₅₀ of 31 nM. Onalespib also strongly inhibits the proliferation of a panel of human tumor cell lines, showing IC₅₀ of < 100 nM^[1]. Onalespib exhibits cytotoxic activity against many of the PPTP cell lines, with median IC₅₀ of 41 nM^[2].

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

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (122.09 mM; ultrasonic and warming and heat to 60°C; 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	2.4419 mL	12.2094 mL	24.4188 mL
5 mM	0.4884 mL	2.4419 mL	4.8838 mL
10 mM	0.2442 mL	1.2209 mL	2.4419 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 16.67 mg/mL (40.71 mM); Suspended solution; Need ultrasonic

Purity & Documentation

Purity: 99.92%

Data Sheet (277 KB) SDS (393 KB)

COA (247 KB) HNMR (140 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Woodhead AJ, et al. Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. J Med Chem. 2010 Aug 26;53 [Content Brief]

[2]. Kang MH, et al. Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Jul 15;59(1):185-8. [Content Brief]

Goat anti-Human IgG Fc, TRITC conjugated

Cat# AS101197

Brand : Agrisera

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