Bezuclastinib

Bezuclastinib (CGT9486) is an orally active, highly selective tyrosine kinase inhibitor with potent activity against KIT D816V. Bezuclastinib can be used for the research of nonadvanced systemic mastocytosis (NonAdvSM) [1].

Product Specifications

CAS Number

[1616385-51-3]

Product Name Alternative

CGT9486; PLX 9486

UNSPSC

12352005

Target

C-Kit

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bezuclastinib.html

Purity

98.81

Solubility

DMSO : 80 mg/mL (ultrasonic)

Smiles

O=C(C1=NNC(C)=C1C)NC2=CN=C3NC(C4=CC=CC=C4)=CC3=C2

Molecular Formula

C19H17N5O

Molecular Weight

331.37

References & Citations

[1]Guarnieri A, et al. Preclinical Data with KIT D816V Inhibitor Bezuclastinib (CGT9486) Demonstrates High Selectivity and Minimal Brain Penetrance. Blood. 2021, 138: 4595. |[2]Guarnieri A, et al. Preclinical data identifies bezuclastinib as a differentiated KIT inhibitor with unique selectivity to KIT D816V and minimal evidence of brain penetration. MOLECULAR CANCER THERAPEUTICS. 2021, 20 (12) .