PF 477736

CAS No. : 952021-60-2

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Cat. No. : HY-10032
M.Wt: 419.48
Formula: C22H25N7O2
Purity: >98 %
Storage: at 20℃ 2 years
Solubility: 10 mM in DMSO
Introduction of 952021-60-2 :

PF 477736 is a potent, selective ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, 100-fold selectivity versus Chk2 (Ki, 47 nM). IC50 & Target: Ki: 0.49 nM (Chk1), 47 nM (Chk2), 9.9 μM (CDK1)[1][2] In Vitro: PF 477736 (PF-00477736, 0.01-1 μM) abrogates the camptothecin-induced DNA damage checkpoint in a dose-dependent manner in CA46 cells. PF 477736 (180, 360, 540 nM) enhances gemcitabine-induced cytotoxicity in a time- and dose-dependent manner in HT29 cells as determined by cell survival assay. PF 477736 (360 nM) in combination with gemcitabine significantly decreases the phosphorylation of CDK1, consistent with checkpoint abrogation and cell entry into mitosis[1]. PF 477736 (PF-00477736) poorly inhibits CDK1 activity, with Ki of 9.9 μM[1][2]. In Vivo: PF 477736 (PF-00477736, 4-60 mg/kg, i.p.) once a day (s.i.d.) or twice a day (b.i.d.) treatment alone exhibits no antitumor activity in human colon Colo205 xenograft model. However, PF 477736 dependently enhances the antitumor activity of a MTD of gemcitabine. PF 477736 (15 and 30 mg/kg) induces histone H3 phosphorylation and DNA damage and increases apoptosis in Colo205 tumor samples from in vivo xenograft model[1].

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