product name GDC-0152
References: J Med Chem. 2012 May 10;55(9):4101-13.
498.64
Formula
C25H34N6O3S
CAS No.
873652-48-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 99 mg/mL (198.5 mM)
Water: 3 mg/mL (6.0 mM)
Ethanol: 99 mg/mL (198.5 mM)
Solubility (In vivo)
30% Propylene glycol, 5% Tween 80, 65% D5W: 5mg/mL
Chemical Name
(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-(4-phenylthiadiazol-5-yl)pyrrolidine-2-carboxamide
other peoduct :
| GDC-0152 can block protein−protein interactions that involve IAP proteins and pro-apoptotic molecules. Using transiently transfected HEK293T cells, GDC-0152 is shown to disrupt XIAP binding to partially processed caspase-9 and to disrupt the association of ML-IAP, cIAP1, and cIAP2 with Smac. | |
|---|---|
| In Vivo | GDC-0152 has moderate predicted hepatic clearance based on metabolic stability assays conducted using human liver microsomes. Plasma−protein binding of GDC-0152 is moderate and comparable among mice (88−91%), rats (89−91%), dogs (81−90%), monkeys (76−85%), and humans (75−83%) over the range of concentrations investigated (0.1−100 μM); higher plasma−protein binding is observed in rabbits (95−96%). |
| Animal model | Human-tumor xenograft mouse models of MDA-MB-231 breast cancer |
| Formulation & Dosage | phosphate-buffered saline; 10, 50, 100 mg/kg; Oral |
| References | [1] Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113. |
