CAS NO: | 1003311-62-3 |
规格: | ≥98% |
Molecular Formula: C23H17N5O2
Exact Mass: 395.1382
Molecular Weight: 395.422
Synonym: AMG25; AMG 25; AMG-25
IUPAC/Chemical Name: 3-(2-Aminoquinazolin-6-yl)-4-methyl-1-[4-(1,3-oxazol-2-yl)phenyl]pyridin-2-one
InChi Key: IGFSMGCBFTXTJK-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C1C(C2=CC3=CN=C(N)N=C3C=C2)=C(C)C=CN1C4=CC=C(C5=NC=CO5)C=C4
In Vitro | 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]. |
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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 ngoh/mL) Cmax(1230 ng/mL), T1/2 (2.6 h), and F (39%) in rats[1]. |
References | [1] 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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