A selective inhibitor of checkpoint kinase 1
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PF-477736

Item No. 17859

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αR)-amino-N-[5,6-dihydro-2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-1H-pyrrolo[4,3,2-ef][2,3]benzodiazepin-8-yl]-cyclohexaneacetamide
CAS Number
952021-60-2
Molecular Formula
C22H25N7O2
Formula Weight
419.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
λmax
265, 330 nm
SMILES
O=C([C@H](N)C1CCCCC1)NC2=CC3=C4C(NC(C5=CN(C)N=C5)=C4C=NNC3=O)=C2
InChi Code
InChI=1S/C22H25N7O2/c1-29-11-13(9-25-29)20-16-10-24-28-21(30)15-7-14(8-17(27-20)18(15)16)26-22(31)19(23)12-5-3-2-4-6-12/h7-12,19,27H,2-6,23H2,1H3,(H,26,31)(H,28,30)/t19-/m1/s1
InChi Key
NDEXUOWTGYUVGA-LJQANCHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $117

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    10 mg

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    25 mg

    $456

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    50 mg

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    Product Description

    PF-477736 is an ATP-competitive inhibitor of Chk1 with a Ki value of 0.49 nM that demonstrates 100-fold selectivity over Chk2.1 When used in combination with various chemotherapeutics, PF-477736 abrogates DNA damage-induced cell cycle arrest, potentiating the antiproliferative effects of these compounds in tumor cell lines and xenografts.1,2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Blasina, A., Hallin, J., Chen, E., et al. Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1. Mol. Cancer Ther. 7(8), 2394-2404 (2008).

    2. Zhang, C., Yan, Z., Painter, C.L., et al. PF-00477736 mediates checkpoint kinase 1 signaling pathway and potentiates docetaxel-induced efficacy in xenografts. Clin. Cancer Res. 15(14), 4630-4640 (2009).

    3. Nguyen, T., Hawkins, E., Kolluri, A., et al. Synergism between bosutinib (SKI-606) and the Chk1 inhibitor (PF-00477736) in highly imatinib-resistant BCR-ABL+ leukemia cells. Leuk. Res. 39, 65-71 (2015).