Chemical Structure : HBC-12551
CAS No.:
2963606-09-7
HBC-12551
(HBC12551)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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660.75
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Formula
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C34H41FN8O5
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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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(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
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References
1. Gang Liu, et al. J Med Chem. 2026 Jan 30. doi: 10.1021/acs.jmedchem.5c02785.
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