HBC-12551 | BTK inhibitor | Probechem Biochemicals

Chemical Structure : HBC-12551

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HBC-12551 (HBC12551)

货号: PC-26002Not For Human Use, Lab Use Only.

HBC-12551 is a potent, selective and noncovalent Bruton's tyrosine kinase (BTK) inhibitor with SPR Kd of 0.25 nM.

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生物&药学活性

HBC-12551 is a potent, selective and noncovalent Bruton's tyrosine kinase (BTK) inhibitor with SPR Kd of 0.25 nM.
HBC-12551 shows potent inhibition of Tyr223 phosphorylation (IC50 = 1.31 nM and IC50 = 2.18 nM, respectively) in HEK293 cells expressing constitutively active wide-type or C481S mutant BTK.
HBC-12551 decreases viability of a panel of malignant B cells (TMD8, TMD8-BTK-C481S, OCI-Ly10, REC-1) with IC50 of 0.95-2.18 nM.
HBC-12551 also significantly inhibited BTK-mediated B cell activation, as indicated by CD69 expression (IC50 = 0.95 nM), in PBMCs.
HBC-12551 (10-20 mg/kg dose (p.o., QD, 14 days)) exhibited great tumor growth inhibition (TGI) efficacy in xenograft mouse models bearing TMD8 and TMD8-BTK-C481S tumors.

物理化学性质&存储条件

分子量	660.75
分子式	C34H41FN8O5
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-(4-((5-Fluoro-2-methoxybenzamido)methyl)phenyl)-4-((6-(1-methoxyethyl)-5-(4-(2-methoxyethyl)piperazin-1-yl)pyridin-2-yl)amino)-1H-pyrazole-5-carboxamide

参考文献

1. Gang Liu, et al. J Med Chem. 2026 Jan 30. doi: 10.1021/acs.jmedchem.5c02785.

HBC-12551 (HBC12551)

生物&药学活性

物理化学性质&存储条件

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HBC-12551 (HBC12551)

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物理化学性质&存储条件

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