1229705-06-9

Basic information

• Product Name: RG-7388
• Synonyms: RG 7388;RG7388;RG-7388;Idasanutlin;4-[[[(2R,3S,4R,5S)-3-(3-Chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl]carbonyl]amino]-3-methoxybenzoic acid;Idasanutlin (RG-7388);RG-7388, Idasanutlin;Pexidartinib Hydrochloride
• CAS NO: 1229705-06-9
• Molecular Formula: C₃₁H₂₉Cl₂F₂N₃O₄
• Molecular Weight: 616.4824664
• Product Categories: Inhibitors
• Mol File: 1229705-06-9.mol
• Article Data: 5

Chemical Properties

• Boiling Point: 737.3±60.0 °C(Predicted)
• Appearance: /
• Density: 1.40±0.1 g/cm3(Predicted)
• Storage Temp.: -20°C Freezer
• Solubility: DMSO (Slightly), Methanol (Slightly)
• PKA: 4.11±0.10(Predicted)
• CAS DataBase Reference: RG-7388(CAS DataBase Reference)
• NIST Chemistry Reference: RG-7388(1229705-06-9)
• EPA Substance Registry System: RG-7388(1229705-06-9)

Safety Data

• Hazardous Substances Data: 1229705-06-9(Hazardous Substances Data)

Usage

Description

RG-7388, also known as Idasanutlin, is a potent MDM2 inhibitor that plays a crucial role in anti-cancer treatments. It has an IC50 of 6 nM in binding assay and 30 nM in cancer cell proliferation assay. RG-7388 induces p53 stabilization, cell cycle arrest, and apoptosis in cancer cells expressing wildtype p53. It also displays inhibition of tumor growth in the SJSA1 tumor xenograft model and inhibits MDR-1 at high concentrations.

Uses

Used in Anticancer Applications:
RG-7388 is used as an anti-cancer agent for blocking the p53 protein-protein interaction, which is essential in the development and progression of various types of cancer. By inhibiting MDM2, RG-7388 stabilizes the p53 protein, leading to cell cycle arrest and apoptosis in cancer cells expressing wildtype p53.
Used in Drug Delivery Systems:
In the pharmaceutical industry, RG-7388 is used as a potent MDM2 inhibitor for developing novel drug delivery systems to enhance its applications and efficacy against cancer cells. Researchers are exploring various organic and metallic nanoparticles as carriers for RG-7388 delivery, aiming to improve its delivery, bioavailability, and therapeutic outcomes.

Upstream product

• 1219086-87-9 (Z)-3-(3-chloro-2-fluorophenyl)-2-(4-chloro-2-fluorophenyl)prop-2-enenitrile 
• 1219086-34-6 2-[(E)-(3,3-dimethylbutylidene)amino]acetic acid tert-butyl ester 
• 75279-53-7 2-(4-chloro-2-fluoro-phenyl)acetonitrile 
• 85070-48-0 2-fluoro-3-chlorobenzaldehyde 
• 2987-16-8 3,3-dimethylbutyrylaldehyde 
• 1219089-31-2 (2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)pyrrolidine-2-carboxylic acid 
• 1229705-05-8 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)pyrrolidine-2-carbonyl]amino}-3-methoxybenzoic acid methyl ester 
• 1606132-23-3 4-(2-aminoacetylamino)-3-methoxybenzoic acid ethyl ester hydrochloride 
• 41608-64-4 methyl 3-methoxy-4-aminobenzoate 
• 1345866-83-2 4-{2-[3,3-dimethyl-but-(E)-ylideneamino]acetylamino}-3-methoxybenzoic acid methyl ester 

Downstream Products

• 1364612-29-2 4-[(5S,6R,7S,7aR)-7-(3-chloro-2-fluorophenyl)-6-(4-chloro-2-fluorophenyl)-6-cyano-5-(2,2-dimethylpropyl)-1-oxo-tetrahydropyrrolo[1,2-c]imidazol-2-yl]-3-methoxybenzoic acid 
• 1364612-62-3 4-[(5S,6R,7S,7aR)-7-(3-chloro-2-fluorophenyl)-6-(4-chloro-2-fluorophenyl)-6-cyano-5-(2,2-dimethylpropyl)-1-oxo-tetrahydropyrrolo[1,2-c]imidazol-2-yl]-3-methoxybenzamide 
• 1456545-74-6 2-((1-(4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoyloxy)ethoxy)carbonylamino)acetic acid 
• 1456545-46-2 1-(cyclohexyloxycarbonyloxy)ethyl 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoate 
• 1456545-72-4 1-(2-(benzyloxy)-2-oxoethylcarbamoyloxy)ethyl 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoate 
• 1456545-41-7 4-methyl-piperazine-1-carboxylic acid 1-(4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoyloxy)-ethyl ester 
• 1456545-63-3 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid 1-{2-[2-(2-methoxy-ethoxy)-ethoxy]-ethoxycarbonyloxy}-ethyl ester 
• 1456545-65-5 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid 1-(2-{2-[2-(2-methoxy-ethoxy)-ethoxy]-ethoxy}-ethoxycarbonyloxy)-ethyl ester 
• 1456545-67-7 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid 1-[2-(2-{2-[2-(2-methoxy-ethoxy)-ethoxy]-ethoxy}-ethoxy)-ethoxycarbonyloxy]-ethyl ester 
• 1456545-81-5 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid benzyloxycarbonylmethyl-carbamoyloxymethyl ester 
• 1456545-83-7 (S)-Dibenzyl 2-(((4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoyloxy)methoxy)carbonylamino)-pentanedioate 
• 1456545-93-9 C₄₆H₅₇Cl₂F₂N₃O₁₃ 
• 1456545-94-0 27-Oxo-2,5,8,11,14,17,20,23,26,28-decaoxatriacontan-29-yl 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoate 
• 1456545-96-2 24-Oxo-2,5,8,11,14,17,20,23,25-nonaoxaheptacosan-26-yl 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoate 

Relevant articles and documents

PHOTORESPONSIVE NUTLIN DERIVATIVES AND USES THEREOF

The invention relates to the field of medicine and medicinal chemistry, more in particular to the design, manufacture and use of anti-cancer drugs that can be activated by an external stimulus that can be applied in a spatiotemporal fashion. Provided herein is a compound having the chemical structure or a pharmaceutically acceptable salt thereof.

Practical Synthesis of MDM2 Antagonist RG7388. Part 2: Development of the Cu(I) Catalyzed [3 + 2] Asymmetric Cycloaddition Process for the Manufacture of Idasanutlin

A concise catalytic asymmetric synthesis of idasanutlin (1) was developed in which the key pyrrolidine core, containing four contiguous stereocenters, was constructed via a Ag/MeOBIPHEP promoted [3 + 2] cycloaddition reaction. Further development of the [

Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development

Restoration of p53 activity by inhibition of the p53-MDM2 interaction has been considered an attractive approach for cancer treatment. However, the hydrophobic protein-protein interaction surface represents a significant challenge for the development of s