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Chemical Structure : TK-642
Catalog No.: 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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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.
| M.Wt | 389.91 | |
| Formula | C17H20ClN7S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Kai Tang, et al. Acta Pharm Sin B. 2024 Aug;14(8):3624-3642.
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