Defactinib, Potent FAK inhibitor (TBI4828)

Description

Product Details

Formal Name: N-Methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]aminl]benzamide

Molecular Formula: C₂₀H₂₁F₃N₈O₃S

Formula Weight: 510.50

CAS Number: 1073154-85-4

Purity: >98%

Formulation: powder

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

Storage: -20°C

Stability: ≥ 1 year.

 

Applications

Potent FAK inhibitor

 

Functions

Defactinib (1073154-85-4) is a potent inhibitor of FAK (IC50 = 0.6nM) and Pyk2 (IC50 = 0.6nM). It is active in vivo (EC50 = 26nM). FAK inhibition prevents tumor invasion and dissemination rather than tumor size reduction. Defactinib has been shown to preferentially target cancer stem cells in a mouse xenograft model of triple negative breast cancer. It is in multiple clinical trials for various cancers and in shows synergistic activity when used in combination with checkpoint immunotherapy.

 

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.

Additional information

SIZE (mg)	25 MG, 5 MG

TBI4828_Defactinib