Product Name

Spebrutinib

General description

Spebrutinib is a covalent, orally active, and highly selective BTK inhibitor with IC50 of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed.

Synonym

CC-292; LMK-435; AVL-292

Purity

≥98.5%(HPLC)

CAS Number

1202757-89-8

Formula

C²²H²²FN⁵O³

Molecular Weight

423.44

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

Solid

Solubility(25°C)

DMSO

≥50mg/ml

Ethanol

Insoluble

Water

Very slightly soluble

l  Biological Information

Biochem/Physiol  Actions

Spebrutinib is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity. Upon administration, spebrutinib targets and covalently binds to BTK, thereby preventing its activity. By irreversibly inhibiting BTK, administration of this agent may lead to an inhibition of B cell receptor (BCR) signaling and may inhibit cell proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.

l  Storage

Storage temp.

-20°C

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov