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产品名称 | ALK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
ASP3026 |
+
ALK, IC50: 3.5 nM |
99%+ | |||||||||||||||||
ALK-IN-1 |
++++
ALK, IC50: 0.07 nM |
98+% | |||||||||||||||||
Crizotinib |
++++
ALK, IC50: 24 nM ROS1, Ki: <0.025 nM |
98% | |||||||||||||||||
Entrectinib | ✔ | 99%+ | |||||||||||||||||
Brigatinib |
+++
ALK, IC50: 0.37 nM ROS1, IC50: 1.9 nM |
FLT3 | 98% | ||||||||||||||||
NVP-TAE 684 |
+
ALK, IC50: 3 nM |
99%+ | |||||||||||||||||
Alectinib |
++
ALK, IC50: 1.9 nM ALK (F1174L), IC50: 3.5 nM |
98% | |||||||||||||||||
Ceritinib |
+++
ALK, IC50: 0.2 nM |
Insulin Receptor,IGF-1R | 98% | ||||||||||||||||
GSK1838705A |
+++
ALK, IC50: 0.5 nM |
Insulin Receptor,IGF-1R | 99% | ||||||||||||||||
AZD-3463 |
++
ALK, Ki: 0.75 nM |
IGF-1R | 99% | ||||||||||||||||
Lorlatinib |
++++
ROS1, Ki: <0.07 nM ALK (L1196M), Ki: 0.07 nM |
98% | |||||||||||||||||
Repotrectinib |
+
ALK(L1196M), IC50: 1.01 nM ALK(G1202R), IC50: 1.26 nM |
Src | 99% | ||||||||||||||||
Belizatinib |
++
ALK, IC50: 0.7 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Anaplastic lymphoma kinase (ALK), a member of the insulin receptor tyrosine kinase family (RTK), is encoded by the ALK gene on chromosome 2p23[1]. Belizatinib is a potent, dual ALK and TrkA, TrkB and TrkC inhibitor which has high affinity for wild-type recombinant ALK kinase activity with an IC50 value of 0.7 nM, and exerts sustained potent inhibition of ALK-dependent tumour growth in mouse models. In an ongoing phase I/IIa trial, Belizatinib exerted antitumour activity in at least 2/3 non-small cell lung cancer (NSCLC) ALK+ patients with dysaesthesia who had previously progressed on crizotinib[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.73mL 0.35mL 0.17mL |
8.65mL 1.73mL 0.87mL |
17.31mL 3.46mL 1.73mL |
CAS号 | 1357920-84-3 |
分子式 | C33H44FN5O3 |
分子量 | 577.733 |
别名 | TSR-011 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 300 mg/mL(519.27 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |