PF-00477736( PF00477736 | PF-477736 )

Catalog No. M16807 CAS No. 952021-60-2

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

Get Quotation Bulk Inquiry Add to Cart

Product Name

PF-00477736
Note

Research use only, not for human use.
Brief 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).
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-fold selectivity over VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret, and Yes in a panel of >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.
In Vitro

——
In Vivo

——
Synonyms

PF00477736 | PF-477736
Pathway

Angiogenesis
Target

Chk
Recptor

c-Fms|Chk1|Chk2|VEGFR2|Yes
Research Area

Cancer
Indication

Solid Tumors

CAS Number

952021-60-2
Formula Weight

419.489
Molecular Formula

C22H25N7O2
Purity

>98% (HPLC)
Solubility

DMSO: 31.5 mg/mL (75 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )
SMILES

CN1C=C(C=N1)C2=C3C=NNC(=O)C4=C3C(=CC(=C4)NC(=O)C(C5CCCCC5)N)N2
Chemical Name

(R)-2-amino-2-cyclohexyl-N-(5-(1-methyl-1H-pyrazol-4-yl)-1-oxo-2,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl)acetamide

1. Blasina A, et al. Mol Cancer Ther. 2008 Aug;7(8):2394-404. 2. Zhang C, et al. Clin Cancer Res. 2009 Jul 15;15(14):4630-40.

Calculator

molnova catalog