PF 477736

CAT: 0804-HY-10032-01Size: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-10032-01Size:1 mg
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
Aurora A; CDK1; Chk1; Chk2; VEGFR2/KDR/Flk-1
Citation 01
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;53 (9) :1390-1401.

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