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Navtemadlin

Catalog No. TQ0127 CAS 1352066-68-2

Synonyms: AMG232, CS-1300

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.

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Navtemadlin, CAS 1352066-68-2

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Purity: 98%

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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

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: Insoluble

DMSO: 45mg/mL (79.15mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Canon J, et al. The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents. Mol Cancer Ther. 2015 Mar;14(3):649-58. 2. Rew Y, et al. Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer. J Med Chem. 2014 Aug 14;57(15):6332-41.

Related compound libraries

This product is contained In the following compound libraries：

Ubiquitination Compound Library

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Navtemadlin M435-1279 Subasumstat SAR405838 Cbl-b-IN-3 YH239-EE Siremadlin NAcM-OPT

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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.

Keywords

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

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