SCH900776 (MK-8776)

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.