PF-00477736

SKU: orb1223534

Description

PF-00477736 (PF-477736) is a potent, selective, ATP-competitive inhibitor of Chk1 with Ki of 0.49 nM, also inhibits Chk2 (Ki=47 nM) and poorly inhibits CDK1 activity (Ki=9.9 uM); displays 100 protein kinases; abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin; enhances the antitumor activity of gemcitabine in a dose-dependent manner in xenografts.Solid Tumors Phase 1 Discontinued.

Key Properties

• CAS Number: 952021-60-2
• MW: 419.489
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₅N₇O₂
• SMILES: CN1C=C(C=N1)C2=C3C=NNC(=O)C4=C3C(=CC(=C4)NC(=O)C(C5CCCCC5)N)N2
• Target: Chk
• Solubility: DMSO: 31.5 mg/mL (75 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PF00477736 | PF-477736

Quick Database Links

Gene Symbol

Chk