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CYC-116

Catalog No. T6458   CAS 693228-63-6

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
CYC-116 Chemical Structure
CYC-116, CAS 693228-63-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 51.00
10 mg In stock $ 72.00
25 mg In stock $ 148.00
50 mg In stock $ 250.00
100 mg In stock $ 450.00
1 mL * 10 mM (in DMSO) In stock $ 59.00
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Purity: 96.6%
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Biological Description
Chemical Properties
Storage & Solubility Information
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:8 nM(Ki), Aurora B:9.2 nM(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)
Molecular Weight 368.46
Formula C18H20N6OS
CAS No. 693228-63-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 23 mg/mL (62.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences 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:
Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Antidepressant Compound Library Anti-Pancreatic Cancer Compound Library Cell Cycle Compound Library MAPK Inhibitor Library Autophagy Compound Library Oxidation-Reduction Compound Library

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Keywords

CYC-116 693228-63-6 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic MAPK PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors VEGFR FLT CDK S6 Kinase Aurora Kinase inhibit Inhibitor CYC116 CYC 116 inhibitor

 

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