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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Anaplastic Lymphoma Kinase (ALK)-Repotrectinib
Repotrectinib

Chemical Structure : Repotrectinib

CAS No.: 1802220-02-5

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Repotrectinib (TPX-0005, Ropotrectinib ,TPX0005)

货号: PC-62298Not For Human Use, Lab Use Only.

Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor, effectively inhibits a broad spectrum of mutations including solvent front ALK G1202R, ROS1 G2032R and TRKA G595R mutants.

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10 mg ￥1180 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
100 mg ￥5280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor, effectively inhibits a broad spectrum of mutations including solvent front ALK G1202R, ROS1 G2032R and TRKA G595R mutants.
Repotrectinib (TPX-0005) potently inhibits WT ALK (IC50=1.01 nM) and mutant ALKs including ALK G1202R (IC50=1.26 nM) and ALK L1196M (IC50=1.08 nM).
Repotrectinib (TPX-0005) is also a potent SRC inhibitor (IC50=5.3 nM); shows low nano-molar activities against CD74-ROS1 G2032R (IC50=8.4 nM), LMNA-TRKA G595R (IC50=0.4 nM),TEL-TRKB G639R (IC50=1.9 nM) and TEL-TRKC G623R (IC50=0.4 nM) in Ba/F3 cell proliferation assays; dramatically causes tumor growth inhibition and tumor regression in xenograft tumor model.
Repotrectinib (TPX-0005) demonstrates desired druglike properties and good safety profile.

物理化学性质&存储条件

分子量 355.373
分子式 C18H18FN5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(7S,13R)-11-fluoro-6,7,13,14-tetrahydro-7,13-dimethyl-1,15-etheno-1H-pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one

参考文献

1. Zhai D, et al. DOI: 10.1158/1538-7445.AM2016-2132 Published July 2016

2. J.J. Cui, et al. DOI: http://dx.doi.org/10.1016/S0959-8049(16)32675-2.

3. Drilon A, et al. Cancer Discov. 2018 Aug 9. pii: CD-18-0484.

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