c-Kit-IN-5-1

Modify Date: 2024-01-08 08:42:53

c-Kit-IN-5-1 Structure
c-Kit-IN-5-1 structure
Common Name c-Kit-IN-5-1
CAS Number 1003311-62-3 Molecular Weight 395.413
Density 1.4±0.1 g/cm3 Boiling Point 720.7±70.0 °C at 760 mmHg
Molecular Formula C23H17N5O2 Melting Point N/A
MSDS N/A Flash Point 389.7±35.7 °C

 Use of c-Kit-IN-5-1


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].

 Names

Name 3-(2-Amino-6-quinazolinyl)-4-methyl-1-[4-(1,3-oxazol-2-yl)phenyl]-2(1H)-pyridinone
Synonym More Synonyms

 c-Kit-IN-5-1 Biological Activity

Description 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].
Related Catalog
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].
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].
References

[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.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 720.7±70.0 °C at 760 mmHg
Molecular Formula C23H17N5O2
Molecular Weight 395.413
Flash Point 389.7±35.7 °C
Exact Mass 395.138214
LogP 2.78
Vapour Pressure 0.0±2.3 mmHg at 25°C
Index of Refraction 1.709
Storage condition -20°C

 Safety Information

Hazard Codes Xn

 Synonyms

2(1H)-Pyridinone, 3-(2-amino-6-quinazolinyl)-4-methyl-1-[4-(2-oxazolyl)phenyl]-
3-(2-Amino-6-quinazolinyl)-4-methyl-1-[4-(1,3-oxazol-2-yl)phenyl]-2(1H)-pyridinone
AMG-25