HBC-12551 

HBC-12551 is an orally active BTK inhibitor (IC₅₀ in HEK293 cells: 1.31 nM for BTK; 2.18 nM for BTK^C481S). HBC-12551 has antitumor activity against diffuse large B-cell lymphoma^[1].

HBC-12551 potently inhibits the phosphorylation of BTK (IC₅₀ = 1.31 nM) and the phosphorylation of the BTK^C481S mutant in HEK293 cells^[1].
HBC-12551 (72 h) potently reduces the cell viability of malignant B-cell lines TMD8 (IC₅₀ = 1.40 nM), TMD8-BTK-C481S (IC₅₀ = 1.92 nM), OCI-Ly10 (IC₅₀ = 1.86 nM) and REC-1 (IC₅₀ = 3.11 nM) after 72 h of incubation^[1].
HBC-12551 (30 min) potently inhibits B cell activation in human peripheral blood mononuclear cells (PBMCs), with an IC₅₀ of 0.95 nM for CD69 expression^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HBC-12551 (10-20 mg/kg; p.o.; QD; 14 days) demonstrates potent dose-dependent tumor growth inhibition in TMD8 xenografts, with 97.2% TGI at 10 mg/kg p.o. QD and 112.8% TGI (tumor regression) at 20 mg/kg p.o. QD over 14 days^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

660.74

C₃₄H₄₁FN₈O₅

2963606-11-1

FC(C=C1)=CC(C(NCC(C=C2)=CC=C2N(N=C3)C(C(N)=O)=C3NC(C=C4)=NC([C@@H](C)OC)=C4N(CC5)CCN5CCOC)=O)=C1OC

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Liu G, et al. Strategic Use of Benzylic Alcohols Reveals Cryptic Hydrogen-Bonding Interactions: Discovery of HBC-12551 as a Potent Noncovalent Bruton's Tyrosine Kinase Inhibitor. J Med Chem. 2026;69(3):2867-2887.  [Content Brief]