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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Trk Receptor-CH7057288
CH7057288

Chemical Structure : CH7057288

CAS No.: 2095616-82-1

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CH7057288 (CH-7057288, CH 7057288)

货号: PC-35679Not For Human Use, Lab Use Only.

CH7057288 (CH-7057288) is a novel potent and selective pan-TRK inhibitor with IC50 of 1.1/7.8/5.1 nM for TRKA/TRKB/TRKC, respectively.

规格 价格 库存 数量
5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3480 In stock
50 mg ￥5280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CH7057288 (CH-7057288) is a novel potent and selective pan-TRK inhibitor with IC50 of 1.1/7.8/5.1 nM for TRKA/TRKB/TRKC, respectively.
CH7057288 shows excellect selectivity, binds to only 6 kinases the KINOMEscan panel (403 non-mutant and 65 mutant kinases) at 100 nM.
CH7057288 suppresses TRK signaling and proliferation of TRK fusion-driven cancer cell (CUTO3, IC50= 9 nM), but not that of TRK-negative cell lines.
CH7057288 significantly induces tumor regression and improves event-free survival in an intracranial implantation model mimicking brain metastasis, maintaines similar levels of in vitro and in vivo activity against one of these resistant mutants as it did to wild‑type TRK.

物理化学性质&存储条件

分子量 569.676
分子式 C32H31N3O5S
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

N-(tert-butyl)-2-((6,6-dimethyl-8-(methylsulfonamido)-11-oxo-6,11-dihydronaphtho[2,3-b]benzofuran-3-yl)ethynyl)-6-methylisonicotinamide

参考文献

1. Tanaka H, et al. Mol Cancer Ther. 2018 Sep 21. pii: molcanther.1180.2017. doi: 10.1158/1535-7163.MCT-17-1180.

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