GRADE & PURITY 10mM in DMSO

Synonyms

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-methoxy-benzoic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Idasanutlin (RG-7388) Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.
In vitro

Idasanutlin inhibits cell proliferation with IC50 of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53.

In vivo

In a mouse SJSA human osteosarcoma xenograft model, Idasanutlin (25 mg/kg p.o.) causes tumor growth inhibition and regression. In a SJSA xenograft model, Idasanutlin results in induction of apoptosis and antiproliferation.
Cell Data

cell lines：primary and immortalized KS cells

Concentrations：~10 μM

Incubation Time：24 hours

Powder Purity:≥99%

Specifications

Synonyms

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-methoxy-benzoic acid

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Mechanism of action

Tumour suppressor p53/oncoprotein Mdm2 inhibitor

Product Properties

• ALogP: 4.3

Names and Identifiers

• Isomeric SMILES: CC(C)(C)C[C@H]1[C@]([C@H]([C@@H](N1)C(=O)NC2=C(C=C(C=C2)C(=O)O)OC)C3=C(C(=CC=C3)Cl)F)(C#N)C4=C(C=C(C=C4)Cl)F
• PubChem CID: 53358942
• Molecular Weight: 616.48

Associated Targets(Human)

MDM2 Tchem E3 ubiquitin-protein ligase Mdm2 (3 Activities)

Discover Target: MDM2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

References

1. Kang Chen, Xiu Xin, Lipeng Qiu, Wenpan Li, Guannan Guan, Gang Li, Mingxi Qiao, Xiuli Zhao, Haiyang Hu, Dawei Chen.  (2019)  Co-delivery of p53 and MDM2 inhibitor RG7388 using a hydroxyl terminal PAMAM dendrimer derivative for synergistic cancer therapy.  Acta Biomaterialia,      [PMID:31568878] [10.1016/j.actbio.2019.09.041]