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

CYC-116 [693228-63-6]

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Cat# HY-10558-10mg

Size : 10mg

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CYC-116 is a potent aurora A and aurora B inhibitor with K_is of 8 and 9 nM, respectively.

For research use only. We do not sell to patients.

CYC-116 Chemical Structure

CAS No. : 693228-63-6

This product is a controlled substance and not for sale in your territory.

Based on 3 publication(s) in Google Scholar

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Aurora Kinase Aurora A Aurora B Aurora C

Description

CYC-116 is a potent aurora A and aurora B inhibitor with K_is of 8 and 9 nM, respectively.

IC₅₀ & Target^[1]

Aurora A

8 nM (Ki)

Aurora B

9.2 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	170 nM Compound: 18, CYC-116	Cytotoxicity against human A2780 cells after 96 hrs by MTT assay Cytotoxicity against human A2780 cells after 96 hrs by MTT assay	[PMID: 20462263]
A549	IC₅₀	0.48 μM Compound: 18, CYC-116	Inhibition of Aurora kinase in human A549 cells assessed as concentration required for half-maximal inhibition of histone H3 serine-10 phosphorylation after 7 hrs immunofluorescence microscopy Inhibition of Aurora kinase in human A549 cells assessed as concentration required for half-maximal inhibition of histone H3 serine-10 phosphorylation after 7 hrs immunofluorescence microscopy	[PMID: 20462263]
BXPC-3	IC₅₀	1.626 μM Compound: 18, CYC-116	Cytotoxicity against human BxPC3 cells after 96 hrs by MTT assay Cytotoxicity against human BxPC3 cells after 96 hrs by MTT assay	[PMID: 20462263]
CCRF-CEM	IC₅₀	0.471 μM Compound: 18, CYC-116	Cytotoxicity against human CCRF-CEM cells after 96 hrs by MTT assay Cytotoxicity against human CCRF-CEM cells after 96 hrs by MTT assay	[PMID: 20462263]
COLO 205	IC₅₀	0.241 μM Compound: 18, CYC-116	Cytotoxicity against human COLO205 cells after 96 hrs by MTT assay Cytotoxicity against human COLO205 cells after 96 hrs by MTT assay	[PMID: 20462263]
HCT-116	IC₅₀	0.34 μM Compound: 18, CYC-116	Cytotoxicity against human HCT116 cells after 96 hrs by MTT assay Cytotoxicity against human HCT116 cells after 96 hrs by MTT assay	[PMID: 20462263]
HeLa	IC₅₀	0.59 μM Compound: 18, CYC-116	Cytotoxicity against human HeLa cells after 96 hrs by MTT assay Cytotoxicity against human HeLa cells after 96 hrs by MTT assay	[PMID: 20462263]
HL-60	IC₅₀	0.372 μM Compound: 18, CYC-116	Cytotoxicity against human HL60 cells after 96 hrs by MTT assay Cytotoxicity against human HL60 cells after 96 hrs by MTT assay	[PMID: 20462263]
HT-29	IC₅₀	0.725 μM Compound: 18, CYC-116	Cytotoxicity against human HT-29 cells after 96 hrs by MTT assay Cytotoxicity against human HT-29 cells after 96 hrs by MTT assay	[PMID: 20462263]
HuP-T4	IC₅₀	0.775 μM Compound: 18, CYC-116	Cytotoxicity against human HUPT4 cells after 96 hrs by MTT assay Cytotoxicity against human HUPT4 cells after 96 hrs by MTT assay	[PMID: 20462263]
K562	IC₅₀	1.375 μM Compound: 18, CYC-116	Cytotoxicity against human K562 cells after 96 hrs by MTT assay Cytotoxicity against human K562 cells after 96 hrs by MTT assay	[PMID: 20462263]
MCF7	IC₅₀	0.599 μM Compound: 18, CYC-116	Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay	[PMID: 20462263]
MES-SA	IC₅₀	0.09 μM Compound: 18, CYC-116	Cytotoxicity against human MESSA cells after 96 hrs by MTT assay Cytotoxicity against human MESSA cells after 96 hrs by MTT assay	[PMID: 20462263]
MIA PaCa-2	IC₅₀	278 nM Compound: 18, CYC-116	Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay	[PMID: 20462263]
MV4-11	IC₅₀	0.034 μM Compound: 18, CYC-116	Cytotoxicity against human MV4-11 cells after 96 hrs by MTT assay Cytotoxicity against human MV4-11 cells after 96 hrs by MTT assay	[PMID: 20462263]
NCI-H460	IC₅₀	0.681 μM Compound: 18, CYC-116	Cytotoxicity against human NCI-H460 cells after 96 hrs by MTT assay Cytotoxicity against human NCI-H460 cells after 96 hrs by MTT assay	[PMID: 20462263]
SAOS-2	IC₅₀	0.11 μM Compound: 18, CYC-116	Cytotoxicity against human Saos2 cells after 96 hrs by MTT assay Cytotoxicity against human Saos2 cells after 96 hrs by MTT assay	[PMID: 20462263]

In Vitro

CYC-116 also inhibits VEGFR2, Src, Lck AND FLT3 with with K_is of 44, 82, 280, 44 nM, respectively. CYC-116 may have broad-spectrum antitumor activity. CYC-116 shows potent antiproliferative activity against cancer cell lines with with IC₅₀s of 0.599, 0.59, 0.241, 0.34, 0.725, 1.375, 0.471, 0.034, 0.372, 0.681, 0.151, 1.626, 0.775, 0.308, 0.110, 0.09 for MCF7, HeLa, Colo205, HCT-116, HT29, K562, CCRF-CEM, MV4-11, HL60, NCI-H460, A2780, BxPC3, HuPT4, Mia-Paca-2, Saos-2, Messa cells. Treatment with 1.25 μM CYC-116 for 7 h results in complete inhibition of histone H3 phosphorylation in HeLa cell lysates^[1].

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

In Vivo

Oral administration of CYC-116 at dose levels of 75 and 100 mg/kg q.d. causes tumor growth delays of 2.3 and 5.8 days, which translates into specific growth delays of 0.32 and 0.81, respectively. The mean relative tumor volumes of mice receiving CYC-116 at both dose levels are less than those of vehicle-treated mice for the duration of the study period. At 100 mg/kg po q.d., the reduction in growth is statistically significant on days 6 and 9^[1].

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

Clinical Trial

Molecular Weight

368.46

Formula

C₁₈H₂₀N₆OS

CAS No.

693228-63-6

Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=C(SC(N)=N1)C2=NC(NC3=CC=C(C=C3)N4CCOCC4)=NC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 15 mg/mL (40.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7140 mL	13.5700 mL	27.1400 mL
5 mM	0.5428 mL	2.7140 mL	5.4280 mL
10 mM	0.2714 mL	1.3570 mL	2.7140 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.

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 40% PEG300 5% Tween-80 45% Saline
Solubility: 1.5 mg/mL (4.07 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.0 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: ≥ 1.5 mg/mL (4.07 mM); Clear solution

This protocol yields a clear solution of ≥ 1.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.0 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.

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).

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: 99.03%

Select Batch:

SDS (393 KB)

COA (246 KB) HNMR (204 KB) RP-HPLC (260 KB) LCMS (147 KB)

Handling Instructions (2659 KB)

References

[1]. Wang S, et al. Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010 Jun 10;53(11):4367-78. [Content Brief]

Kinase Assay ^[1]	Aurora A kinase assays are performed using a 25 μL reaction volume (25 mM β-glycerophosphate, 20 mM Tris/HCl, pH 7.5, 5 mM EGTA, 1 mM DTT, 1 mM Na₃VO₄, 10 μg of kemptide (peptide substrate)), and recombinant aurora A kinase is diluted in 20 mM Tris/HCl, pH 8, containing 0.5 mg/mL BSA, 2.5% glycerol, and 0.006% Brij-35. Reactions are started by the addition of 5 μL Mg/ATP mix (15 mM MgCl₄, 100 μM ATP, with 18.5 kBq γ-³²P-ATP per well) and incubated at 30°C for 30 min before terminating by the addition of 25 μL of 75 mM H₃PO₄. Aurora B kinase assays are performed as for aurora A except that prior to use, aurora B is activated in a separate reaction at 30°C for 60 min with inner centromeres protein^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay	CYC-116 is prepared in DMSO and diluted in cell medium^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: Mice implanted intraperitoneally with P388/0 cells are treated with CYC-116, and the antitumor activity is measured as an increase in lifespan of the treated animals versus the vehicle control group^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Wang S, et al. Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010 Jun 10;53(11):4367-78. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.7140 mL	13.5700 mL	27.1400 mL	67.8500 mL
	5 mM	0.5428 mL	2.7140 mL	5.4280 mL	13.5700 mL
	10 mM	0.2714 mL	1.3570 mL	2.7140 mL	6.7850 mL
	15 mM	0.1809 mL	0.9047 mL	1.8093 mL	4.5233 mL
	20 mM	0.1357 mL	0.6785 mL	1.3570 mL	3.3925 mL
	25 mM	0.1086 mL	0.5428 mL	1.0856 mL	2.7140 mL
	30 mM	0.0905 mL	0.4523 mL	0.9047 mL	2.2617 mL
	40 mM	0.0678 mL	0.3392 mL	0.6785 mL	1.6962 mL

CYC-116 Related Classifications

Cell Cycle/DNA Damage Epigenetics
Aurora Kinase

CYC-116 [693228-63-6]

Cat# HY-10558-10mg

Brand : MedChemExpress

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CYC-116 Related Classifications

Keywords:

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CYC-116 [693228-63-6]

Cat# HY-10558-10mg

Brand : MedChemExpress

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Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CYC-116 Related Classifications

Keywords:

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