pf06463922
cas no. 1454846-35-5
英文品名 pf-06463922
中文品名 pf-06463922
分子式 c21h19fn6o2
分子量 406.15
规格/纯度 98%
供应能力 can supply g scale
别名 pf 06463922;pf06463922
产品简述 pf-06463922 is a novel, orally available, cns-penetrant, atp-competitive inhibitor of alk/ros1 with ki of <0.02 nm, <0.07 nm, and 0.7 nm for ros1, alk (wt), and alk (l1196m), respectively.
详细说明 pf-06463922 demonstrates significant cell activity against alk and a large set of alk clinical mutations with ic50 ranging from 0.2 nm-77 nm. pf-06463922 exhibited subnanomolar cellular potency against oncogenic ros1 fusions and inhibited the crizotinib-refractory ros1(g2032r) mutation and the ros1(g2026m) gatekeeper mutation. compared with crizotinib and the second-generation alk/ros1 inhibitors ceritinib and alectinib, pf-06463922 showed significantly improved inhibitory activity against ros1 kinase. in vivo: pf-06463922 showed marked antitumor activity in tumor models expressing fig-ros1, cd74-ros1, and the cd74-ros1(g2032r) mutation. furthermore, pf-06463922 demonstrated antitumor activity in a genetically engineered mouse model of fig-ros1 glioblastoma.
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湖北帝鑫化工制造有限公司

15172426395
中国 武汉