KIN-8194 | HCK BTK inhibitor | Probechem Biochemicals

Chemical Structure : KIN-8194

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KIN-8194 (KIN8194)

货号: PC-72484Not For Human Use, Lab Use Only.

KIN-8194 (KIN8194) is a highly potent dual HCK and BTK inhibitor with IC50 of <0.495 and 0.915 nM, respectively.

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生物&药学活性

KIN-8194 (KIN8194) is a highly potent dual HCK and BTK inhibitor with IC50 of <0.495 and 0.915 nM, respectively.
KIN-8194 demonstrated greater selectivity compared with A419259 with no KIT, RET, PDGFRA, EPHB6, or CDPK1 inhibition.
KIN-8194 binds to gatekeeper residue Thr333 of HCK, but not to Cys481 of BTK.
KIN-8194 shows robust inhibition of both HCK and BTK activity in MYD88-mutated cells, showed robust inhibition of HCK Tyr410 phosphorylation; inhibits the growth and survival of MYD88-mutated WM and ABC DLBCL cells.
KIN-8194 overcomes ibrutinib resistance relatedto BTK Cys481Ser-expressing MYD88-mutated B-cell lymphoma cells, synergizes with the BCL-2 inhibitor venetoclax.
KIN-8194 shows superior activity over ibrutinib in MYD88-mutated TMD-8 ABC DLBCL xenograft mouse model.
KIN-8194 is active against ibrutinib resistance in BTK Cys481Ser -expressing ABC DLBCL xenograft mouse model.

物理化学性质&存储条件

分子量	483.62
分子式	C28H33N7O
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-((1r,4r)-4-(4-methylpiperazin-1-yl)cyclohexyl)-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

参考文献

1. Guang Yang, et al. Blood. 2021 Nov 18;138(20):1966-1979.

KIN-8194 (KIN8194)

生物&药学活性

物理化学性质&存储条件

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KIN-8194 (KIN8194)

生物&药学活性

物理化学性质&存储条件

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