Idasanutlin (RG-7388) - 10mM in DMSO , Tumour suppressor p53/oncoprotein Mdm2 inhibitor, CAS No.1229705-06-9, Tumour suppressor p53/oncoprotein Mdm2 inhibitor

CAS: 1229705-06-9 Cat. No.: I409284 Peso molecular: 616.48 Número EC: 833-504-1 PubChem CID: 53358942

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

Descripción general

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

Sinónimos

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

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Mecanismo de acción

Tumour suppressor p53/oncoprotein Mdm2 inhibitor

Propiedades del producto

• ALogP: 4.3

Nombres e identificadores

• Isómeros 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
• Peso molecular: 616.48

Objetivos asociados (humanos)

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)

Referencias

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]