CYC-116

SKU: orb1300751

Description

CYC116 is a potent, selective dual Aurora A/B kinase inhibitor (Ki = 8.0/9.2 nM) with weaker activity against VEGFR2 and minimal off-target effects on other key kinases. It has been utilized in preclinical research to investigate cell cycle disruption and antitumor efficacy in both cellular and animal models.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 693228-63-6
• MW: 368.46
• Purity: 97.59%
• Formula: C₁₈H₂₀N₆OS
• SMILES: Cc1nc(N)sc1-c1ccnc(Nc2ccc(cc2)N2CCOCC2)n1
• Target: S6 Kinase,CDK,Aurora Kinase,FLT,VEGFR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:13.4 mg/mL (36.37 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  Aurora B:9.2 nM(Ki)|Aurora A:8 nM(Ki)
• 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.
• 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. 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. 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AuroraKinase, Aurora Kinase, Aurora B, Aurora A, CYC 116, CYC116, CYC-116, CDK2/CyclinE, CDK9/CyclinT, p70 S6K, Inhibitor, inhibit, FLT3, S6Kinase, S6 Kinase, VEGFR2

Compound Identifiers

PubChem CID

6420138