TK-642 | SHP2 inhibitor | Probechem Biochemicals

Chemical Structure : TK-642

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TK-642 (TK642)

货号: PC-23044Not For Human Use, Lab Use Only.

TK-642 is a highly potent, selective, orally bioavailable, allosteric SHP2 inhibitor with IC50 of 2.7 nM (SHP2WT) and Ki of 1.53 nM.

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生物&药学活性

TK-642 is a highly potent, selective, orally bioavailable, allosteric SHP2 inhibitor with IC50 of 2.7 nM (SHP2WT) and Ki of 1.53 nM.
TK-642 exhibits negligible inhibitory activity against SHP2PTP (1.5% inhibition at 10 μmol/L).
TK-642 shows notable selectivity toward SHP2 over SHP2PTP, SHP1 and PTP1B, with IC50 values > 100 μmol/L.
TK-642 may competitively bind to the same "tunnel"-like allosteric pocket in SHP2 as SHP099.
TK-642 inhibits cell proliferation and induces apoptosis of esophageal cancer cells in vitro (KYSE-52 cell, IC50=5.73 nM), via suppressing SHP2-mediated AKT and ERK signaling pathways.
TK-642 (50 mg/kg) suppresses tumor growth of esophageal cancer in KYSE-520 xenograft esophageal cancer models.

物理化学性质&存储条件

分子量	389.91
分子式	C17H20ClN7S
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	1-[3-[(3-Chloro-4-pyridinyl)thio]-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl-4-piperidinemethanamine

参考文献

1. Kai Tang, et al. Acta Pharm Sin B. 2024 Aug;14(8):3624-3642.

TK-642 (TK642)

生物&药学活性

物理化学性质&存储条件

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TK-642 (TK642)

生物&药学活性

物理化学性质&存储条件

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