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PF 477736
$42 – $552
Products Details
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 <100-fold selectivity for Chk1 over 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].
Web ID
– HY-10032
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular 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
SMILES
– O=C([C@@H](C1CCCCC1)N)NC2=CC3=C(C(C=NNC4=O)=C(N3)C5=CN(N=C5)C)C4=C2
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– DMSO : 125 mg/mL (ultrasonic)
Target
– Aurora Kinase;CDK;c-Fms;Checkpoint Kinase (Chk);FGFR;FLT3;RET;Src;VEGFR
Isoform
– Aurora A;CDK1;Chk1;Chk2;FGFR3;VEGFR2/KDR/Flk-1
Pathway
– Cell Cycle/DNA Damage;Epigenetics;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
