ChemicalBook > CAS DataBase List > SAR405838 (MI-773)

SAR405838 (MI-773)

Product Name: SAR405838 (MI-773)
CAS No.: 1303607-60-4
Chemical Name: SAR405838 (MI-773)
Synonyms: MI 77301;SAR405838;SAR405838 (MI-773);MI-773 (SAR405838);SAR405838, MI-77301;MI-77301 (SAR405838);Inhibitor (sar405838);SAR405838（1303607-60-4）;SAR405838, 10 mM in DMSO;SAR405838 (MI-773) USP/EP/BP
CBNumber: CB42736431
Molecular Formula: C29H34Cl2FN3O3
Formula Weight: 562.5
MOL File: 1303607-60-4.mol

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SAR405838 (MI-773) Property

Boiling point:: 732.1±60.0 °C(Predicted)
Density: 1.36±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: ≥17.2 mg/mL in DMSO
form: Powder
pka: 12.03±0.70(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML2772
Product name: SAR405838
Purity: ≥98% (HPLC)
Packaging: 1mg
Price: $68.78
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML2772
Product name: SAR405838
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $268
Updated: 2025/07/31

Cayman Chemical

Product number: 17473
Product name: MI-77301
Purity: ≥95%
Packaging: 500μg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 17473
Product name: MI-77301
Purity: ≥95%
Packaging: 1mg
Price: $74
Updated: 2024/03/01

Cayman Chemical

Product number: 17473
Product name: MI-77301
Purity: ≥95%
Packaging: 5mg
Price: $235
Updated: 2024/03/01

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SAR405838 (MI-773) Chemical Properties,Usage,Production

Description

The protein p53, often called the ‘guardian of the genome,’ is a transcription factor that is activated in response to cellular stress (low oxygen levels, heat shock, DNA damage, etc.) and acts to prevent further proliferation of the stressed cell by promoting cell cycle arrest or apoptosis. Its role as a tumor suppressor is evident by the observation that approximately 50% of human tumors have mutated or non-functional p53. Mdm2, a key negative regulator of p53, which is over-expressed in many human tumors, functions by binding to and targeting p53 for proteasomal degradation. MI-77301 binds to MDM2 with a K_i value of 0.88 nM and blocks the MDM2-p53 interaction. It activates wild-type p53 in vitro and in xenograft tumor tissue of leukemia and solid tumors, leading to p53-dependent cell cycle arrest and/or apoptosis. In an SJSA-1 xenograft model of osteosarcoma, a single dose of 200 mg/kg MI-77301 induces complete tumor regression in mice by upregulating the pro-apoptotic protein PUMA.

Uses

MI-773 is aninhibitors of MDM2-p53 protein-protein interaction (MDM2 inhibitors), currently investigated in clinical trials for cancer treatment.

in vivo

At well-tolerated dose schedules, SAR405838 achieves either durable tumor regression or complete tumor growth inhibition in mouse xenograft models of SJSA-1 osteosarcoma, RS4;11 acute leukemia, LNCaP prostate cancer and HCT-116 colon cancer. Remarkably, a single oral dose of SAR405838 is sufficient to achieve complete tumor regression in the SJSA-1 model. 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].

References

[1]. wang s, sun w, zhao y, et al. sar405838: an optimized inhibitor of mdm2-p53 interaction that induces complete and durable tumor regression. cancer res, 2014, 74(20): 5855-5865.

SAR405838 (MI-773) Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from SAR405838 (MI-773) manufacturers

Career Henan Chemical Co

Product: SAR 405838 1303607-60-4
Price: US $1.00/KG
Min. Order: 1KG
Purity: Min98% HPLC
Supply Ability: g/kg/ton
Release date: 2020-01-01

1303607-60-4, SAR405838 (MI-773)Related Search:

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SAR405838 (MI-773)

(2'S,3R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-N-(trans-4-hydroxycyclohexyl)-2-oxo-spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide

MI-773 (SAR405838)

SAR405838;SAR-405838;SAR 405838

MI-77301 (SAR405838)

SAR405838

SAR405838, MI-77301

MI 77301

Spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide, 6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-N-(trans-4-hydroxycyclohexyl)-2-oxo-, (2'S,3R,4'S,5'R)-

SAR405838 (MI-773) USP/EP/BP

MI-773 (2'S,3R isomer, SAR-405838)

Inhibitor (sar405838)

MI773|||MI 773|||MI-77301|||MI-773

SAR405838, 10 mM in DMSO

SAR405838（1303607-60-4）

1303607-60-4

Inhibitors