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Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
PF-477736;PF 477736
12
爱必信(上海)生物科技有限公司
952021-60-2
25mg/5mg/50mg/10mg
规格: | 25mg | 产品价格: | ¥2674.0 |
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规格: | 5mg | 产品价格: | ¥1019.0 |
规格: | 50mg | 产品价格: | ¥5072.0 |
规格: | 10mg | 产品价格: | ¥1706.0 |
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抑制剂描述: 产品名称:PF-477736 产品别名:见爱必信官网 英文别名:PF-477736 靶点:Chk CAS:952021-60-2 纯度:>98% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 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。 溶解性:DMSO :31.5 mg/mL (75 mM) 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. 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. 产品信息订购:
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