PF06463922原料藥供應(yīng)-當(dāng)日16：00發(fā)貨
 
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

規(guī)格/純度 98%
供應(yīng)能力 can supply g scale
別名  PF 06463922;PF06463922
產(chǎn)品簡(jiǎn)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.
詳細(xì)說明 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.

3922還可以抑制ros1靶點(diǎn)，其作用力是alk的3倍，是目前ros1的2代藥。

3922 應(yīng)該是目前最廣譜及活性的ALK/ROS抑制劑。它是微堿性，胃溶性稍高一些。它的腸吸收率高，即使腸溶也應(yīng)不錯(cuò)。腸溶的副反應(yīng)會(huì)小一些。胃溶腸溶都可以，空腹服用。

1.PF06463922的起始劑量有腦轉(zhuǎn)的從25mg吃起，沒有腦轉(zhuǎn)的從20mg吃起，如果無效的話，每10mg劑量遞增。

2.PF06463922對(duì)腦轉(zhuǎn)的控制能力很強(qiáng)，25mg劑量足以入腦。

3.PF06463922有心臟毒性，試驗(yàn)組有2人因心臟毒性不能吃更高的劑量。輔酶Q10每天要服用，建議密切關(guān)注心電圖QTC時(shí)間，超過450ms要引起注意。

4.PF06463922會(huì)引起間質(zhì)性肺炎，服用初期不要一下使用高劑量。

5.PF06463922可能和克唑替尼有同樣的肝臟毒性，水飛薊建議服用，密切檢測(cè)肝功能。

6.試驗(yàn)組號(hào)病人是克唑替尼耐藥后吃LDK378，LDK378耐藥后服用3922，每天25mg，目前效果很好。