| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | c-Kit-IN-5-1 | ||||||||||||
| CAS | 1003311-62-3 | ||||||||||||
| Formula | C23H17N5O2 | ||||||||||||
| Molar Mass | 395.41 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |
c-Kit-IN-5-1
CAS: 1003311-62-3 F: C23H17N5O2 W: 395.41
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-K
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