PF 477736

PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively) . PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo[1][2].

Product Specifications

CAS Number

[952021-60-2]

Product Name Alternative

PF 00477736

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Aurora Kinase; CDK; c-Fms; Checkpoint Kinase (Chk) ; FGFR; FLT3; RET; Src; VEGFR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PF-477736.html

Purity

99.04

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C([C@@H](C1CCCCC1)N)NC2=CC3=C(C(C=NNC4=O)=C(N3)C5=CN(N=C5)C)C4=C2

Molecular Formula

C22H25N7O2

Molecular Weight

419.48

Precautions

H302, H315, H319, H335

References & Citations

[1]Blasina A, et al. Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1. Mol Cancer Ther. 2008 Aug;7 (8) :2394-404|[2]Ashwell S, et, al. DNA damage detection and repair pathways--recent advances with inhibitors of checkpoint kinases in cancer therapy. Clin Cancer Res. 2008 Jul 1; 14 (13) : 4032-7.