ChemicalBook--->CAS DataBase List--->2489226-14-2

2489226-14-2

2489226-14-2 Structure

2489226-14-2 Structure
IdentificationBack Directory
[Name]

AZD4747
[CAS]

2489226-14-2
[Synonyms]

AZD4747
[Molecular Formula]

C24H22ClFN2O3
[MOL File]

2489226-14-2.mol
[Molecular Weight]

440.9
Chemical PropertiesBack Directory
[Boiling point ]

612.703±55.00 °C(Press: 760.00 Torr)(predicted)
[density ]

1.404±0.10 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
[form ]

Solid
[pka]

7.898±0.40(predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRASG12C inhibitor. AZD4747 has the potential to study cancer[1].
[in vivo]

AZD4747 (1.1-2.3 μM/kg (i.v.); 2.3-6.8 μM/kg (p.o.); single) shows clearances of moderate to high, with 52 and 75% of hepatic blood flow for the mouse and rat, respectively[1].

Animal Model:Male CD1 mice, male Wistar Han rats[1].
Dosage: Mouse: 2.3 μM/kg (i.v.); 6.8 μM/kg (p.o.);
Rat: 1.1-2.3 μM/kg (i.v.); 6.8 μM/kg (p.o.).
Administration:i.v. and p.o.
Result:1.19Pharmacokinetic Parameters of AZD4747 in Cross Species[1].
MouseRat
IVaPOaIVaPOa
Eh (%)5275
Vss (L/kg)2.91.7
T1/2 (h)0.630.56
F%5818
Note:
a: 5% DMSO, 95% SBE-B-CD (30% w/v) in water.
[References]

[1] Kettle JG, et al. Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration. J Med Chem. 2023 Jul 13;66(13):9147-9160. DOI:10.1021/acs.jmedchem.3c00746
Spectrum DetailBack Directory
[Spectrum Detail]

AZD4747(2489226-14-2)1HNMR
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