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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Phosphatase/PTP-JAB-3312
JAB-3312

Chemical Structure : JAB-3312

CAS No.: 2245082-05-5

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JAB-3312 (JAB3312)

货号: PC-22889Not For Human Use, Lab Use Only.

JAB-3312 is a potent, selective and allosteric SHP2 inhibitor with binding Kd of 0.37 nM and enzymatic IC50 of 1.9 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

JAB-3312 is a potent, selective and allosteric SHP2 inhibitor with binding Kd of 0.37 nM and enzymatic IC50 of 1.9 nM.
JAB-3312 is inactive in inhibiting other 22 phosphatases (including SHP1 and the PTP domain of SHP2) and 25 kinases.
JAB-3312 exhibits IC50 of 7.4 nM in KYSE-520 antiproliferation assay, and IC50 of 0.23 nM in p-ERK inhibition assay in KYSE-520 cell line.
JAB-3312 (0.1-1 mg/kg, QD, p.o.) exhibited dose-dependent antitumor effects in KYSE-520 and MV-4–11 xenograft models.

物理化学性质&存储条件

分子量 439.97
分子式 C21H22ClN7S
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

(S)-1′-(5-((2-amino-3-chloropyridin-4-yl)thio)pyrazin-2-yl)-5,7-dihydrospiro[cyclopenta[b]pyridine-6,4′-piperidin]-5-amine

参考文献

1. Ma C, et al. J Med Chem. 2024 Aug 7. doi: 10.1021/acs.jmedchem.4c00360.

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