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SAR405838

Name: SAR405838
Brand: TargetMol
SKU: T6585
Price: 45 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6585Cas No. 1303607-60-4

Alias MI-77301, MI-773, MI773, MI 773

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

SAR405838

🥰Excellent

Purity: 98.04%

Catalog No. T6585Alias MI-77301, MI-773, MI773, MI 773Cas No. 1303607-60-4

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

Pack Size	Price	Availability
1 mg	$45	In Stock
2 mg	$83	In Stock
5 mg	$135	In Stock
10 mg	$225	In Stock
25 mg	$441	In Stock
50 mg	$649	In Stock
100 mg	$926	In Stock
500 mg	$1,870	In Stock

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Purity:98.04%

Resource Download

COA ORP FNMR LCMS HNMR

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Product Introduction

Bioactivity

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	SAR405838 binds to MDM2 with Ki of 0.88 nM. SAR405838 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, SAR405838 (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)
Alias	MI-77301, MI-773, MI773, MI 773

Chemical Properties

Molecular Weight	562.5
Formula	C₂₉H₃₄Cl₂FN₃O₃
Cas No.	1303607-60-4
Smiles	CC(C)(C)C[C@@H]1N[C@H]([C@H](c2cccc(Cl)c2F)[C@]11C(=O)Nc2cc(Cl)ccc12)C(=O)N[C@H]1CC[C@H](O)CC1
Relative Density.	1.36 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 93 mg/mL (165.33 mM), Sonication is recommended.

Ethanol: 29 mg/mL (51.56 mM), Sonication is recommended.

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

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7778 mL	8.8889 mL	17.7778 mL	88.8889 mL
5 mM	0.3556 mL	1.7778 mL	3.5556 mL	17.7778 mL
10 mM	0.1778 mL	0.8889 mL	1.7778 mL	8.8889 mL
20 mM	0.0889 mL	0.4444 mL	0.8889 mL	4.4444 mL
50 mM	0.0356 mL	0.1778 mL	0.3556 mL	1.7778 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0178 mL	0.0889 mL	0.1778 mL	0.8889 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

Dose Conversion

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Tech Support

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