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Navtemadlin

Catalog No. TQ0127 CAS 1352066-68-2

Synonyms: AMG232, CS-1300

Navtemadlin (AMG232) 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

Pack Size	Availability	Price/USD
1 mg	In stock	$ 67.00
2 mg	In stock	$ 95.00
5 mg	In stock	$ 147.00
10 mg	In stock	$ 228.00
25 mg	In stock	$ 463.00
50 mg	In stock	$ 683.00
100 mg	In stock	$ 973.00
1 mL * 10 mM (in DMSO)	In stock	$ 188.00

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Purity: 98.86%

ee: 100%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Navtemadlin (AMG232) 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 1 year

Solubility Information

H2O: Insoluble

DMSO: 50 mg/mL (87.94 mM)

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：

Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library HIF-1 Signaling Pathway Compound Library Anti-Lung Cancer Compound Library Apoptosis Compound Library Transcription Factor-Targeted Compound Library PPI Inhibitor Library Anti-Pancreatic Cancer Compound Library

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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 Apoptosis Ubiquitination Mdm2 E1/E2/E3 Enzyme MDM-2/p53 inhibit Ubiquitin ligase Ubiquitin activating enzyme E3 ligating enzyme E2 conjugating enzyme AMG 232 AMG232 Ubiquitin conjugating enzyme AMG-232 KRT232 CS-1300 KRT 232 KRT-232 CS1300 E1 activating enzyme CS 1300 Inhibitor inhibitor

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