PF06463922生产厂家找武汉新百川医药
供应商：武汉新百川医药科技有限公司[查看公司详情]
所在地：武汉市硚口区中山大道
价格：面议
经营模式：
联系人：唐先生
产品简介
PF06463922生产厂家找武汉新百川医药
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PF06463922哪里有？武汉新百川医药有现货
PF06463922哪家工厂生产？武汉新百川医药生产
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PF06463922
CAS NO.
英文品名 PF-06463922
中文品名 PF-06463922劳拉替尼
分子式 C21H19FN6O2
分子量 406.15
规格/纯度 99%
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.
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.
PF06463922国外近研究实验进展有关新闻如下：
3922还可以抑制ros1靶点，其作用力是alk的3倍，是目前ros1的2代药。
3922 应该是目前广谱及活性的ALK/ROS抑制剂。它是微碱性，胃溶性稍高一些。它的肠吸收率高，即使肠溶也应。肠溶的副反应会小一些。胃溶肠溶都可以，空腹服用。
1.PF06463922的起始剂量有脑转的从25mg开始用，没有脑转的从20mg开始用，如果无效的话，每10mg剂量递增。
2.PF06463922对脑转的控制能力很强，25mg剂量足以入脑。
3.PF06463922有心脏毒性，试验组有2人因心脏毒性不能吃更高的剂量。辅酶Q10每天要用，建议密切关注心电图QTC时间，超过450ms要引起注意。
4.PF06463922会引起间质性肺炎，服用初期不要一下使用高剂量。
5.PF06463922可能和克唑替尼有同样的肝脏毒性，水飞蓟建议服用，密切检测肝功能。
6.试验组是克唑替尼耐药后用LDK378，LDK378耐药后用3922，每天25mg，目前效果很好。
新百川医药替尼类新型小分子抑制剂：马来酸来那替尼，曲美替尼，阿法替尼，克唑替尼，苹果酸卡博替尼，阿西替尼，托法替尼，依鲁替尼，鲁索替尼，巴瑞克替尼，色瑞替尼，艾乐替尼，多韦替尼，司美替尼，达克替尼（Dacomitinib，PF299804），PF0643922;劳拉替尼，布格替尼Brigatinib，达沙替尼，替沃扎尼475108-18-0
