| Chemical Properties | Back 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 Information | Back 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].
| Mouse | Rat | | IVa | POa | IVa | POa | | Eh (%) | 52 | | 75 | | | Vss (L/kg) | 2.9 | | 1.7 | | | T1/2 (h) | 0.63 | | 0.56 | | | F% | | 58 | | 18 |
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 |
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