Product Description: 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].
Applications: Cancer-Kinase/protease
Formula: C22H25N7O2
Citations: Cancers. 2019 Oct 25;11(11):1654./Harvard Medical School LINCS LIBRARY/Research Square Preprint. 2022 Jul./Sci Transl Med. 2018 Jul 18;10(450):eaaq1093./Science. 2017 Dec 1;358(6367):eaan4368./Exp Mol Med. 2021 Sep 22.
References: [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.
CAS Number: 952021-60-2
Molecular Weight: 419.48
Compound Purity: 99.21
Research Area: Cancer
Solubility: DMSO : 125 mg/mL (ultrasonic)
Target: Aurora Kinase;CDK;c-Fms;Checkpoint Kinase (Chk);FGFR;FLT3;RET;Src;VEGFR
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