产品名称

SAR405838 - MI-77301

产品货号

Axon 2741 CAS [1303607-60-4] MF C29H34Cl2FN3O3MW 562.50 Purity: 98% Optical purity: Optically pure Soluble in DMSO Description SAR405838 is an inhibitor of the MDM2-p53 interaction with high specificity over other proteins (Ki value of 0.88 nM). SAR405838 effectively 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. 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. KEYWORDS: SAR405838 | supplier | MDM2 inhibitor | MI-77301 | SAR 405838 | SAR-405838 | MI 77301 | MI77301 | CAS [1303607-60-4] | p53 | HDM-MDM | Inhibitor | Enzymes | Apoptosis

产品价格

现货询价，电话：010-67529703

产品规格

产品品牌

axonmedchem

产品概述

产品详情

SAR405838 - MI-77301

Based on 12 reference(s) in Google Scholar 8 10 12

Axon 2741

CAS [1303607-60-4]

MF C29H34Cl2FN3O3
MW 562.50

Purity: 98%
Optical purity: Optically pure
Soluble in DMSO

SAR405838

Description

SAR405838 is an inhibitor of the MDM2-p53 interaction with high specificity over other proteins (Ki value of 0.88 nM). SAR405838 effectively 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. 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.

KEYWORDS: SAR405838 | supplier | MDM2 inhibitor | MI-77301 | SAR 405838 | SAR-405838 | MI 77301 | MI77301 | CAS [1303607-60-4] | p53 | HDM-MDM | Inhibitor | Enzymes | Apoptosis

S Wang et al. SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression. Cancer Res. 2014 Oct 15;74(20):5855-65.

J Jung et al. TP53 mutations emerge with HDM2 inhibitor SAR405838 treatment in de-differentiated liposarcoma. Nat Commun. 2016 Aug 31;7:12609.

M de Jonge et al. A phase I study of SAR405838, a novel human double minute 2 (HDM2) antagonist, in patients with solid tumours. Eur J Cancer. 2017 May;76:144-151.

Apoptosis Cell Cycle Regulation Cell Signaling & Oncology Transcription Factors p53-Tumor Suppression DNA-damage Response Ubiquitin EC 6.3.2.19 HDM-MDM

MDM2-p53 inhibitor

Chemical name

(2'S,3R,4'S,5'R)-6-Chloro-4'-(3-chloro-2-fluorophenyl)-N-((1r,4R)-4-hydroxycyclohexyl)-2'-neopentyl-2-oxospiro[indoline-3,3'-pyrrolidine]-5'-carboxamide

Parent CAS No.

[1303607-60-4]

产品资料