Ibrutinib, BTK inhibitor (TBI4757)

Description

Product Details

Formal Name: 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one

Alternate Names: PCI-32765

Molecular Formula: C₂₅H₂₄N₆O₂

Formula Weight: 440.51

CAS Number: 936563-96-1

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

BTK inhibitor

Functions

Ibrutinib (936563-96-1) is a very potent (IC50 = 0.5nM) irreversible inhibitor of Bruton tyrosine kinase (BTK) that blocks activation of the B-cell antigen receptor (BCR). Ibrutinib also potently inhibits several other kinases including BLK, BMS, FGR, EGFR, and ITK. It is a clinically useful drug to treat B cell cancers. It inhibits CLL cell migration and survival and downregulates expression of CD20. It enhanced antitumor immune responses in combination with anti PD-L1 blockade via its inhibition of ITK (IL2-inducible T-cell kinase).

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.