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Cat. No.: HY-181547

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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.

For research use only. We do not sell to patients.

CAS No.: 2963606-11-1
Formula: C₃₄H₄₁FN₈O₅
Molecular Weight:660.74

Storage:

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

Data Sheet (271 KB)

HBC-12551 Chemical Structure

CAS No.: 2963606-11-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Classifications
Bioz

Biological Activity

Description

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].

In Vitro

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.

In Vivo

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.

Animal Model:

CB17 SCID (female)^[1]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

p.o.; QD; 14 days
Result:

Inhibited tumor growth by 97.2% relative to vehicle control.
Resulted in tumor regression with a tumor growth inhibition (TGI) of 112.8%.
Showed no abnormal clinical observations or significant body weight loss in treated mice.

Chemical Information

CAS No. 2963606-11-1
Molecular Weight 660.74
Formula C₃₄H₄₁FN₈O₅
SMILES

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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