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Background Information:
SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of CHK1(IC50 = 3 nM), highly selective against CHK2 (IC50 = 1500 nM) and CDK2 (IC50 = 160 nM).* It is currently in clinical trials.
Reference:
1. T. J. Guzi, et al., Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening. Mol Cancer Ther. 2011 Apr;10(4):591-602.
2. M. Labroli, et al., Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach – part 2. Bioorgan. & Med. Chem.Lett. 2011, 21(1):471-474* The activity of our product, SCH900776 (R-Enantiomer), has been confirmed by head-to-head comparison with the S-Enantiomer. The results are consistent with the reported - R-enantiomer is much more potent and selective than its opposite isomer (S-enantiomer, wrong isomer).
APIM050239: SCH900776 (MK-8776)
CAS No.: 891494-63-6.
Molecular Formula: C15H18BrN7?1.8HCl?0.4H2O.
Molecular Weight: 449.1.
Purity: >99% chem and optical purity (HPLC and chiral HPLC at 215 and 254 nm).
QC: HPLC-MS, 1HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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