c-Kit-IN-5-1

• CAT Number: I021961
• CAS Number: 1003311-62-3
• Molecular Formula: C23H17N5O2
• Molecular Weight: 395.41
• Purity: ≥95%
• Synonyms: 3-(2-aminoquinazolin-6-yl)-4-methyl-1-[4-(1,3-oxazol-2-yl)phenyl]pyridin-2-one
• InChI: InChI=1S/C23H17N5O2/c1-14-8-10-28(18-5-2-15(3-6-18)21-25-9-11-30-21)22(29)20(14)16-4-7-19-17(12-16)13-26-23(24)27-19/h2-13H,1H3,(H2,24,26,27)
• InChIKey: IGFSMGCBFTXTJK-UHFFFAOYSA-N
• SMILES: CC1=C(C(=O)N(C=C1)C2=CC=C(C=C2)C3=NC=CO3)C4=CC5=CN=C(N=C5C=C4)N

c-Kit-IN-5 is potent inhibitor of c-Kit, with IC50s of 22 nM and 16 nM in kinase assay and cell assay, respectively. c-Kit-IN-5 shows more than 200-fold selectivity for c-Kit over KDR, p38, Lck, and Src. c-Kit-IN-5 also exhibits desirable pharmacokinetic properties[1].
c-Kit-IN-5 (compound 25) shows more than 200-fold selectivity against KDR, p38, Lck, and Src (IC50=>5.0, 40, 7.8 , and >5.0 μM, respectively)[1].
c-Kit-IN-5 (compound 25) (1 mg/kg; i.v.) exhibits CL (0.46 L/h/kg) and Vdss (1.59 L/kg) in rats[1].
c-Kit-IN-5 (10 mg/kg; p.o.) exhibits AUC0-t(9860 ng•h/mL) Cmax(1230 ng/mL), T1/2 (2.6 h), and F (39%) in rats[1].

Reference

[1]. Hu E, et, al. Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. J Med Chem. 2008 Jun 12;51(11):3065-8.
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