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Angiogenesis FLT CYC116

CYC116

Catalog No. T6458   CAS 693228-63-6
Purity 96.60% Datasheet

CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.

CYC116, CAS 693228-63-6
Pack Size Availability Price/USD Quantity
10 mg In stock 80.00
25 mg In stock 171.00
50 mg In stock 278.00
100 mg In stock 501.00
200 mg In stock 901.00
1 mL * 10 mM (in DMSO) In stock 69.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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Description CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.
Targets&IC50 Aurora A :ic50 8nM(Ki),   Aurora B :ic50 9nM(Ki),   CDK2/CyclinE :ic50 0.39μM(Ki),   CDK9/CyclinT :ic50 0.48μM(Ki),   FLT3 :ic50 44nM(Ki),   p70 S6K :ic50 Ki:0.54μM ,   VEGFR2 :ic50 44nM(Ki),  
In vitro The most Aurora-selective CYC116 shows inhibitory effect on Aurora A and B kinases 50-fold more potently than any of the CDKs assayed. [1] CYC116 is initially screened against a panel of human leukemia and solid tumor cell lines using an MTT antiproliferative assay. The results show that CYC116 has broad-spectrum antitumor activity and shows specific cytotoxicity against the acute myelogenous leukemia cell line MV4-11 with IC50 of 34 nM. [1] In addition, anti-proliferative activity of CYC116 is found to be associated with Aurora A and B modulation such as, inhibition of Aurora autophosphorylation, reduction of histone H3 phosphorylation, polyploidy, followed by cell death, resulting from a failure in cytokinesis. [1]
In vivo Mice bearing subcutaneous NCI-H460 xenografts are given CYC116 orally for 5 days, at dose levels of 75 and 100 mg/kg q.d. It leads to tumor growth delays of 2.3 and 5.8 days, which translated into specific growth delays of 0.32 and 0.81, respectively. [1]
Kinase Assay Kinase Assays: 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)). 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 MgCl2, 100 μM ATP, with 18.5 kBq γ-32P-ATP per well) and incubated at 30°C for 30 minutes before termination with 25 μL of 75 mM H3PO4. Aurora B kinase assays are performed like Aurora A except that prior to use, Aurora B is activated in a separate reaction at 30°C for 60 minutes with inner centromere protein.
Cell Research
Standard MTT assays are performed. In short, cells are seeded into 96-well plates according to doubling time and incubated overnight at 37°C. Test compounds are made up in DMSO, a 3-fold dilution series is prepared in 100 μL of cell medium, added to cells (in triplicates) and incubated for 72 or 96 hours at 37°C. MTT is made up as a stock of 5 mg/mL in cell medium, and the solution is filter-sterilized. Medium is removed from the cells followed by a wash with PBS. MTT solution is then added at 20 μL/well and incubated in the dark at 37°C for 4 hours. MTT solution is removed and cells are again washed with 200 μL of PBS. MTT dye is solubilized with 200 μL/well of DMSO by agitation. Absorbance is read at 540 nm and data analyzed using curve-fitting software to determine IC50 values. (Only for Reference)
Cell lines: HeLa, MCF7, MV4-11 and A2780 cells
Animal Research
Animal Model: NCI-H460 cells are implanted intraperitoneally into the mice.
Molecular Weight 368.46
Formula C18H20N6OS
CAS No. 693228-63-6

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 23 mg/mL (62.4 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

1% DMSO/30% polyethylene glycol/1% Tween 80: 30 mg/mL

Citations

References and Literature
1. Wang S, et al. J Med Chem. 2010, 53(11), 4367-4378.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Anti-cancer Compound Library Epigenetics Compound Library

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