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产品介绍
产品介绍
产品信息
抗原名称
Chk1 ,VEGFR2 ,Fms ,YES ,Chk2
商品描述
PF-477736是一种有效的，选择性，ATP竞争性Chk1抑制剂，Ki为0.49 nM，也抑制VEGFR2， Aurora-A， FGFR3， Flt3， Fms (CSF1R)， Ret和Yes。作用于Chk1比作用于Chk2选择性高100倍左右。PF 477736(128 nM)作用于CA46 和 HeLa细胞，废除Camptothecin诱导的DNA损伤检查点，这种作用具有剂量依赖性。PF 477736作用于HT29细胞，有效废除Gemcitabine诱导的S期停滞，使凋亡细胞群相应增加。PF 477736(540 nM)作用于HT29细胞，增强Gemcitabine诱导的细胞毒性,这种作用具有时间和剂量依赖性。
分子量
419.48
纯度
>98%
可溶性
DMSO ：31.5 mg/mL (75 mM)
In vitro(体外研究)
PF-477736 (128 nM) abrogates the camptothecin-induced DNA damage checkpoint in a dose-dependent manner in CA46 and HeLa cells. PF-477736 effectively abrogates the gemcitabine-induced S-phase arrest with a corresponding increase in apoptotic cell populations in HT29 cells. PF-477736 (540 nM) enhances gemcitabine-induced cytotoxicity in a time- and dose-dependent manner in HT29 cells. PF-477736 potentiates the growth-inhibitory activity of a panel of chemotherapeutic agents across a broad spectrum of p53-deficient human cancer cell lines in the MTT assay. Addition of PF-477736 (360 nM) to gemcitabine-arrested cells induces a dramatic increase in the intensity of H2AX phosphorylation, reflecting a greater number of γ-H2AX molecules near sites of DNA damage. PF-477736 (0.5 nM) selectively blocks p73 and P53 phosphorylation in presence of curcumin in HL-60 cells. PF-477736 (360 nM) suppresses docetaxel-induced phosphorylation of histone H3 (Ser10) and Cdc25C (Ser216) and potentiates apoptosis in COLO205 cells. PF-477736 (250 nM) combined with MK-1775 has marked synergistic cytotoxic activity in OVCAR-5 cells. PF-477736 (250 nM) combined with MK-1775 causes accumulation of cells with a DNA content between 2N and 4N in OVCAR-5 cells. PF-477736 (250 nM) combined with MK-1775 causes premature mitosis before the end of DNA replication, with damaged DNA leading to apoptotic cell death in OVCAR-5 cells.
In vivo(体内研究)
PF-477736 (4 mg/kg i.v.) results in terminal half-life (T1/2) of 2.9 hours, AUC of 5.72 μg×hr/mL and CLp of 11.8 mL/min/kg in rats. PF-477736 dose-dependently enhances the antitumor activity of a maximum tolerated dose of gemcitabine in the Colo205 xenograft mouse model. PF-477736 (12 mg/kg) induces an increase in the phosphorylation of histone H3 (Ser10) and of phospho-histone H2AX in the Colo205 xenograft mouse model. PF-477736 (15 mg/kg i.p.) enhances docetaxel induced tumor growth inhibition and tumor growth delay in COLO205 and MDA-MB-231 xenograft models. PF 477736 (10 mg/kg once daily i.p.) combined with MK-1775 (30 mg/kg twice a day oral) leads to greater tumor growth inhibition in mice bearing OVCAR-5 xenografts.
背景
别名
PF 477736
分子式
C22H25N7O2
CAS号
952021-60-2
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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