PF-0477736 ≥95%
Supplier: ADIPOGEN CORP MS
Synonyms:
PF-0477736, (R)-α-Amino-N-[5,6-dihydro-2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-1H-pyrrolo[4,3,2-ef][2,3]benzodiazepin-8-yl]-cyclohexaneacetamide
Antagonizing the Chk1-mediated cell cycle checkpoints has emerged as an attractive target for anticancer therapy. If Chk1 activity is blocked, DNA-damaged or spindle-disrupted cells would exit cell cycle arrest before full repair and subsequently undergo mitotic catastrophe or cell death. Chk1 inhibitors consequently increase the therapeutic index of DNA-damaging or antimitotic agents as well. PF-0477736 is a selective, potent ATP-competitive Chk1 inhibitor, derived from PF-0394691, inhibits Chk1 (Ki, 0.49nM) and Chk2 (Ki, 47nM) in vitro. In tests, PF-0477736 was identified as a potent, selective ATP-competitive small-molecule inhibitor that inhibits Chk1 with a Ki of 0.49nM. PF-0477736 abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin. In xenografts, PF-0477736 enhanced the antitumor activity of gemcitabine in a dose-dependent manner. PF-0477736 combinations were well tolerated with no exacerbation of side effects commonly associated with cytotoxic agents.
Formula:
C₂₂H₂₅N₇O₂ MW: 419.48 g/mol Storage Temperature: Freezer |
MDL Number:
MFCD16038847 CAS Number: 952021-60-2 |
Specification Test Results
Purity |
|
Appearance/Color | Solid. |
Solubility | Soluble in DMSO. |
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