Bezuclastinib

• CAT Number: I045117
• CAS Number: 1616385-51-3
• Purity: ≥95%
• Synonyms: 4,5-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-3-carboxamide
• InChI: InChI=1S/C19H17N5O/c1-11-12(2)23-24-17(11)19(25)21-15-8-14-9-16(22-18(14)20-10-15)13-6-4-3-5-7-13/h3-10H,1-2H3,(H,20,22)(H,21,25)(H,23,24)
• InChIKey: NVSHVYGIYPBTEZ-UHFFFAOYSA-N
• SMILES: CC1=C(NN=C1C(=O)NC2=CN=C3C(=C2)C=C(N3)C4=CC=CC=C4)C

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].
Bezuclastinib (25 mg/kg, p.o., 3 days) shows a brain:plasma ratio of 0.07 in rats[2].
Pharmacokinetic Analysis in Rats[2]

Route
Dose (mg/kg)
t1/2 (h)
Cmax (ng/mL)
AUClast (h*ng/mL)

p.o.
25
2.8
2592±364
21509±2558