武漢帝康醫(yī)藥 原料藥廠家 供應(yīng)優(yōu)質(zhì)AP26113高含量地雜質(zhì) 原料藥

中文名稱：AP26113 
CAS號(hào)：1197958-12-5
含量：99%
分子式：C26H34ClN6O2P
分子量：529.01
作用：AP26113是一種有效的ALK抑制劑，用于ALK突變陽性的非小細(xì)胞肺癌。
存儲(chǔ)條件：2 year -20°C powder, 2 week 4°C in DMSO6 month -80°C in DMSO

AP26113是一種有效的ALK抑制劑，IC50為0.62 nM，可克服由于L1196M突變介導(dǎo)的Crizotinib抵抗作用。AP26113高度有效作用于敏感型和耐藥型H3122細(xì)胞，降低細(xì)胞生長(zhǎng)，抑制ALK磷酸，并誘導(dǎo)細(xì)胞凋亡，這種作用存在劑量依賴性。AP26113作用于H3122 和 H3122 CR 細(xì)胞,降低p-ALK，IC50分別為7.4 和 16.8 nM。AP26113作用于表達(dá)野生型或突變型EML4-ALK的Ba/F3 細(xì)胞，降低細(xì)胞數(shù)，IC50分別為10 nM 和 24 nM。

FDA 授予 Ariad 肺癌藥物 AP26113 突破性治療藥物資格

體外研究：
AP26113 is highly active against both sensitive and resistant H3122 cells, decreasing cell growth, suppressing ALK phosphorylation and inducing apoptosis in a dose dependent manner. AP26113 decreases p-ALK in the H3122 and H3122 CR cells, with IC50 values of 7.4 versus 16.8 nM, respectively. AP26113 decreases cell number in Ba/F3 cells expressing either native or mutant EML4-ALK with IC50 of 10 nM and 24 nM, respectively. AP26113 inhibits cell growth of SU-DHL-1, H3122 and Ba/F3-EML4-ALK v1 cell lines with GI50 of 9 nM, 4 nM and 13 nM, respectively. AP26113 inhibits phosphorylation of ALK with IC50 of 3.2 nM, 1.5 nM and 2.1 nM in Karpas-299, SU-DHL-1 and L-82 cell lines. AP26113 dose-dependently inhibits phosphorylation of ALK and ERK in Karpas-299 and H3122 cells. AP26113 inhibits cell growth with IC50 of 11 nM and 16 nM in Ba/F3 line (native EML4-ALK) and Ba/F3 line (EML4-ALK G1269S mutants). AP26113 inhibits ALK phosphorylationh with IC50 of 74 nM and 335 nM in Ba/F3 line (native EML4-ALK) and Ba/F3 line (EML4-ALK E1210K mutants). AP26113 (10 mg/kg-75 mg/kg) is efficacious in PF-02341066-resistant EML4-ALK mutant mouse xenograft models. AP26113 induces regression of tumors expressing native EML4-ALK and the G1269S and L1196M mutants at 25 mg/kg, 50 mg/kg and 50 mg/kg, respectively. AP26113 inhibits EGFR phosphorylation and viability with IC50 of 75 nM and 114 nM, respectively, in Ba/F3 cells expressing EGFR-DEL. AP26113 inhibits EGFR phosphorylation and viability with IC50s of 15 and 281 nM, respectively, in Ba/F3 cells expressing EGFR-DEL/T790M. AP26113 inhibits EGFR phosphorylation with an IC50 of 62 nM and cell growth with a GI50 of 165 nM in a NSCLC line expressing EGFR-DEL (HCC827). AP26113 inhibits EGFR phosphorylation with an IC50 of 59 nM and cell growth with a GI50 of 245 nM in HCC827 cells expressing EGFR-DEL/T790M. AP26113 potently inhibits SLC34A2-ROS-driven signaling and proliferation in a dose dependent manner in HCC78 NSCLC cells.

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