PF 477736

• 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].

• 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.

• CAS Number:

  [952021-60-2]