Powder: -20°C for 3 years
In solvent: -80°C for 2 years
AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.
Description | AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM. |
Targets&IC50 | MDM2:0.045 nM (Kd), p53-MDM2:0.6 nM |
In vitro | AMG 232 (10 μM) induces p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines [1]. |
In vivo | AMG 232 (10, 25, 75 mg/kg, once daily, p.o.) activates p53 pathway activity in vivo and potently inhibits the growth of tumor xenografts in mice. It also blocks DNA synthesis and induces apoptosis in vivo[1]. AMG 232 causes a dose-dependent tumor growth inhibition with an ED50 of 16 mg/kg [2]. |
Cell Research | Cell Line: SJSA-1, HCT116, ACHN, NCI-H460, MOLM-13, RKO, MCF7, 22RV1, HT-29, PC-3, NCI-H82, NCI-SNU1, MG-63, NCI-H2452, SW982, C32, SK-HEP-1, A375, RT4, RPMI2650, MDA-MB-134-VI, NCI-H2347, and A427 cells. Concentration: 0-10 μM [1]. Incubation Time: 72 hours. |
Animal Research | Animal Model: Female athymic nude mice (n=10) based cancer models. Dosage: 10, 25, 75 mg/kg. Administration: Once daily by oral gavage [1]. |
Synonyms | AMG232, CS-1300 |
Molecular Weight | 568.55 |
Formula | C28H35Cl2NO5S |
CAS No. | 1352066-68-2 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
H2O: Insoluble
DMSO: 45mg/mL (79.15mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Navtemadlin 1352066-68-2 凋亡 泛素化 E1/E2/E3 Enzyme Mdm2 MDM-2/p53 inhibit Ubiquitin ligase Ubiquitin activating enzyme E3 ligating enzyme E2 conjugating enzyme AMG-232 CS-1300 Ubiquitin conjugating enzyme KRT232 KRT 232 AMG232 KRT-232 AMG 232 E1 activating enzyme Inhibitor inhibitor