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SAR405838

Catalog No. T6585 CAS 1303607-60-4

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

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

SAR405838, CAS 1303607-60-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
2 mg	In stock	$ 83.00
5 mg	In stock	$ 135.00
10 mg	In stock	$ 225.00
25 mg	In stock	$ 441.00
50 mg	In stock	$ 649.00
100 mg	In stock	$ 926.00
500 mg	In stock	$ 1,870.00
1 mL * 10 mM (in DMSO)	In stock	$ 166.00

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Purity: 98.04%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MI-773 (SAR405838 (MI 773)) 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 773, MI-77301, MI-773
Molecular Weight	562.5
Formula	C29H34Cl2FN3O3
CAS No.	1303607-60-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (165.3 mM)

Ethanol: 29 mg/mL (51.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Compound Library Bioactive Compound Library Ubiquitination Compound Library Anti-Lung Cancer Compound Library PPI Inhibitor Library

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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 Apoptosis Ubiquitination Mdm2 E1/E2/E3 Enzyme MDM-2/p53 SAR 405838 Ubiquitin activating enzyme MI77301 inhibit MI773 Ubiquitin ligase Inhibitor MI 77301 MI 773 MI-77301 Ubiquitin conjugating enzyme E2 conjugating enzyme SAR-405838 E3 ligating enzyme E1 activating enzyme MI-773 inhibitor

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