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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-Mobocertinib succinate
Mobocertinib succinate

Chemical Structure : Mobocertinib succinate

CAS No.: 2389149-74-8

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Mobocertinib succinate (TAK-788, TAK788)

货号: PC-73154Not For Human Use, Lab Use Only.

Mobocertinib succinate (TAK-788) is a potent, mutant-selective, irreversible inhibitor of EGFR ex20ins mutations with IC50 of 2.7 to 22.5 nM.

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250 mg ￥3480 In stock
1 g ￥6880 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

Mobocertinib succinate (TAK-788) is a potent, mutant-selective, irreversible inhibitor of EGFR ex20ins mutations with IC50 of 2.7 to 22.5 nM.
Mobocertinib (TAK-788) displays selectivity over WT EGFR (IC50=34.5 nM).
Mobocertinib (TAK-788) inhibited all five variants of EGFR ex20ins mutations with IC50 of 4.3 nM for NPG, 10.9 nM for ASV, 11.8 nM for A763_Y764insFQEA (FQEA), 18.1 nM for N771_H773dupNPH (NPH), and 22.5nM for S768_D770dupSVD.
Mobocertinib (TAK-788) inhibited viability of various EGFRex20ins-driven cell lines more potently (CUTO14 cell viability assay, IC50=33 nM) than approved EGFR TKIs and demonstrated in vivo antitumor efficacy in patient-derived xenografts and murine orthotopic models.

物理化学性质&存储条件

分子量 703.8
分子式 C36H45N7O8
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

Isopropyl 2-((5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenyl)amino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate xsuccinate

参考文献

1. Han H, et al. Cancer Res. 2021 Oct 15;81(20):5311-5324.

2. Zhang SS, et al. Lung Cancer (Auckl). 2021 Jul 12;12:61-65.

3. Gonzalvez F, et al. Cancer Discov. 2021 Jul;11(7):1672-1687.

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