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(CAS: 939981-39-2)

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Background Information of RG7112

RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. IC50 Value: Target: MDM2/p53 Restoration of p53 activity by inhibiting the p53-MDM2 interaction may represent a novel approach to cancer treatment.

Solubility of RG7112

Solubility Sources
Soluble in DMSO Apexbio Technology LLC
DMSO MedChemexpress Co., Ltd.

Storage Condition of RG7112

Storage Condition Sources
Store at -20°C Apexbio Technology LLC

MSDS Information

MSDS Sources
MedChemexpress Co., Ltd.

Quality Control and Spectral Data

QC Reports Sources
[HNMR] [NP-HPLC] [LCMS] MedChemexpress Co., Ltd.

Mechanism and Indications

Signaling Pathways Apoptosis
Target MDM-2/p53
Research Area Cancer
Indications Acute myelogenous leukemia Soft tissue sarcoma Cancer Solid tumor Liposarcoma

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
RG7112 Roche Holding AG Acute myelogenous leukemia 2012/7/31 2013/9/30 Phase 1 Clinical
RG7112 Roche Holding AG Soft tissue sarcoma 2012/5/31 2013/8/31 Phase 1 Clinical
RG7112 Roche Holding AG Cancer 2012/11/30 2014/8/31 Phase 1 Clinical
RG7112 Roche Holding AG Solid tumor 2010/8/31 2013/5/01 Phase 1 Clinical
RG7112 Roche Holding AG Liposarcoma 2010/6/30 2011/3/01 Phase 1 Clinical
RG7112 - No Development Reported

Chemical Information

M.Wt Formula CAS No. Synonyms
727.78 C38H48Cl2N4O4S 939981-39-2 RG-7112;RG 7112; ((4S,5R)-2-(4-(tert-butyl)-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethyl-4,5-dihydro-1H-imidazol-1-yl)(4-(3-(methylsulfonyl)propyl)piperazin-1-yl)methanone

Structure Information of RG7112

Smiles C[[email protected]@]1([[email protected]](C)(N(C(C2=CC=C(C=C2OCC)C(C)(C)C)=N1)C(N3CCN(CC3)CCCS(=O)(C)=O)=O)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl
InChI InChI=1S/C38H48Cl2N4O4S/c1-8-48-33-26-29(36(2,3)4)14-19-32(33)34-41-37(5,27-10-15-30(39)16-11-27)38(6,28-12-17-31(40)18-13-28)44(34)35(45)43-23-21-42(22-24-43)20-9-25-49(7,46)47/h10-19,26H,8-9,20-25H2,1-7H3/t37-,38+/m0/s1

Related Products

Other Form Products of RG7112

Name CAS Formula Suppliers
RG7112 Racemate 1313611-29-8 C38H48Cl2N4O4S 1

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Chemical and Physical Properties

Appearance:White to off-white Solid Melting point:
Boiling point: Flash Point:
Water Solubility: Solubility:In vitro:DMSO,100 mg/mL(137.68 mM);In vitro:Ethanol,100 mg/mL(137.68 mM);In vitro:Water,Insoluble;In vivo:Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):1% CMC NaFor best results, use promptly after
Density: Merck:
BRN: Refractive Index:
Vapour: EINECS:
Optical Rotation: alpha:


[1].Vu, Binh; Wovkulich, Peter; Pizzolato, Giacomo et al. Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. ACS Medicinal Chemistry Letters (2013), 4(5), 466-469.
The p53 tumor suppressor is a potent transcription factor that plays a key role in the regulation of cellular responses to stress. It is controlled by its negative regulator MDM2, which binds directly to p53 and inhibits its transcriptional activity. MDM2 also targets p53 for degradation by the proteasome. Many tumors produce high levels of MDM2, thereby impairing p53 function. Restoration of p53 activity by inhibiting the p53-MDM2 interaction may represent a novel approach to cancer treatment. RG7112 (2g) is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. In cancer cells expressing wild-type p53, RG7112 stabilizes p53 and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts.

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