产品说明书

Belizatinib

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Chemical Structure| 1357920-84-3 同义名 : TSR-011
CAS号 : 1357920-84-3
货号 : A288219
分子式 : C33H44FN5O3
纯度 : 99%+
分子量 : 577.733
MDL号 : MFCD31382200
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
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：
生物活性
靶点

  • ALK

    ALK, IC50:0.7 nM
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].
实验方案
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
参考文献

[1]Sullivan I, Planchard D. ALK inhibitors in non-small cell lung cancer: the latest evidence and developments. Ther Adv Med Oncol. 2016 Jan;8(1):32-47. doi: 10.1177/1758834015617355. PMID: 26753004; PMCID: PMC4699265.