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SAR405838

Catalog No. T6585 CAS 1303607-60-4

Synonyms: MI773, MI-77301, MI 773, MI-773

MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

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SAR405838, CAS 1303607-60-4

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
Targets&IC50	MDM2:0.88 nM(Ki)
In vitro	MI-773 binds to MDM2 with Ki of 0.88 nM. MI-773 potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10 μM), PC-3 (IC50, >10 μM), SW620 (IC50, >10 μM), and HCT-116 (p53-/-) (IC50, >20 μM) cells. [1]
In vivo	In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg,). [1]
Kinase Assay	Fluorescence-polarization binding assay: Binding af?nities of MDM2 inhibitors and p53 peptide to MDM2 protein are determined using an Fluorescence-polarization (FP) binding assay. Binding af?nities of MI-773 to Bcl-2, Bcl-xL, Mcl-1, and β-catenin are determined using a competitive FP-based assay, and its binding af?nity to MDMx is determined using Biolayer Interferometry technology.
Cell Research	Cell growth inhibition activity is determined in a water-soluble tetrazolium-based assay. Cell death is measured by trypan blue staining and apoptosis is determined using an Annexin V-FLUOS staining kit.(Only for Reference)

Synonyms	MI773, MI-77301, MI 773, MI-773
Molecular Weight	562.51
Formula	C29H34Cl2FN3O3
CAS No.	1303607-60-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 93 mg/mL (165.3 mM)

Ethanol: 29 mg/mL (51.6 mM)

H2O: <1 mg/mL

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

References and Literature

1. Wang S, et al. Cancer Res. 2014, 74(20), 5855-5865.

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

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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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

SAR405838 1303607-60-4 凋亡泛素化 E1/E2/E3 Enzyme Mdm2 MDM-2/p53 MI773 SAR-405838 Ubiquitin activating enzyme inhibit Ubiquitin ligase Inhibitor MI 77301 SAR 405838 Ubiquitin conjugating enzyme E2 conjugating enzyme E3 ligating enzyme E1 activating enzyme MI-77301 MI 773 MI-773 MI77301 inhibitor

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