Chemical Structure : TK-642
CAS No.:
2765183-10-4
TK-642
(TK642)
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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389.91
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Formula
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C17H20ClN7S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-[3-[(3-Chloro-4-pyridinyl)thio]-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl-4-piperidinemethanamine
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References
1. Kai Tang, et al. Acta Pharm Sin B. 2024 Aug;14(8):3624-3642.
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