| Bioactivity | 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]. | ||||||||||||
| Invitro | PF 477736 is a poor inhibitor of CDK1 activity (Ki=9.9 μM, 20,000-fold versus Chk1)[1].PF 477736 (0.01-1 μM; 16 h) dose-dependently abrogates the camptothecin-induced DNA damage checkpoint in CA46 cells[1].PF 477736 (10-48 h) abrogates the Gemcitabine-induced S-phase arrest and induces increase in apoptotic cell death in HT29 cells[1].PF 477736 (180-540 nM; 4-48 h) enhances Gemcitabine cytotoxicity in dose- and time-dependent manner in HT29 cells[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PF 477736 相关抗体: | ||||||||||||
| In Vivo | PF 477736 (4-60 mg/kg; i.p. for once a day or twice a day for four treatments) potentiates Gemcitabine antitumor activity in Colo205 xenografts[1].PF 477736 (15 and 30 mg/kg; i.p.) induces histone H3 phosphorylation and DNA damage and increases apoptosis in vivo[1].PF 477736 (4 mg/kg; i.v.) exhibits low systemic plasma clearance (11.8 mL/min/kg) and terminal half-life (2.9 h) in rats[1].PF 477736 (4-40 mg/kg; i.p.) exhibits a dose dependent pharmacokinetics[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||
| CAS | 952021-60-2 | ||||||||||||
| Formula | C22H25N7O2 | ||||||||||||
| Molar Mass | 419.48 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [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. |
PF 477736
CAS: 952021-60-2 F: C22H25N7O2 W: 419.48
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
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.