Free shipping on all orders over $ 500

CYC116

Cat. No. M1694
CYC116 Structure
Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 270 In stock
200mg USD 680 In stock
Bulk Inquiry?

Quality Control
Biological Activity

CYC116 is a potent, small molecule inhibitor of Aurora A, B and C with IC50 value of 44, 19 and 65 nM respectively. Additionally, CYC116 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2) kinase in vitro (IC50= 69 nM). CYC116 has antitumor activity in various solid tumor and leukemia xenograft model.

Protocol
Cell Experiment
Cell lines HeLa, MCF7, MV4-11 and A2780 cells line
Preparation method Cell Viability Assay.
Inhibition of cell growth was measured by a standard MTT (thiazolyl blue; 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay using a panel of tumor cell lines.Briefly: cells were seeded (2,500–5,000 cells/well) in 96-well plates and allowed to attach for ~ 24 h. Cells were incubated with test compounds for 96 h in DMEM medium containing 10% fetal bovine serum. Cells were treated with a range of compound concentrations in triplicate to generate dose-response curves. The compound concentration required to inhibit 50% of cell growth (IC50) was determined using nonlinear regression analysis.
Concentrations 0~10 μ M
Incubation time 96 h
Animal Experiment
Animal models Murine P388/D1 Leukemia Model (1) / Murine NCI-H460 non-small cell lung cancer xenograft model (2)
Formulation DMSO/ddH20
Dosages 45 or 67mg/kg twice daily on days 1-3 and 7-9(1) / 75 and 100mg/kg once daily starting on day 1 and for 5 days(2)
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 368.46
Formula C18H20N6OS
CAS Number 693228-63-6
Purity >99%
Solubility DMSO
Storage at -20°C
References

An integrated pharmacokinetic-pharmacodynamic model for an Aurora kinase inhibitor.
Kamei et al. J Pharmacokinet Pharmacodyn. 2010 Aug;37(4):407-34. PMID: 20694801.

Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.
Wang S, et al. J Med Chem. 2010 Jun 10;53(11):4367-78. PMID: 20462263.

Related Aurora Kinase Products
SNS-314

SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively.

GSK1070916

GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex.

PHA-680632

PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.

MK-5108

MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity.

PF-03814735

PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CYC116 supplier, Aurora Kinase, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.