产品名称

SHP099

产品货号

Axon 2633 CAS [1801747-42-1] MF C16H19Cl2N5MW 352.26 Purity: 99% Soluble in DMSO Description Highly potent, selective and orally bioavailable SHP2 inhibitor (IC50 value 0.071 μM) that stabilizes SHP2 in an auto-inhibited conformation. SHP099 potently inhibits ERK phosphorylation and the growth of cancer cell lines that have alterations in RTKs or other tyrosine kinases such as the Janus kinases JAK1 and JAK2. SHP099 showed no detectable activity against a panel of 21 phosphatases and 66 kinases (including the closest homologue SHP1), and only had modest activity against 5HT3 when profiled against a preclinical safety pharmacology panel representing 49 common adverse drug reaction targets. KEYWORDS: SHP099 | supplier | SHP2 inhibitor | SHP-099 | SHP 099 | CAS [1801747-42-1] | [1801747-11-4] | Tyrosine Phosphatase | PTP | PTPN11 | PTP-2C | programmed cell death pathway | PD-1/PD-L1 | Noonan | Leopard | RAS-ERK signaling

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

SHP099

Based on 2 reference(s) in Google Scholar 10 10 2

Axon 2633

CAS [1801747-42-1]

MF C16H19Cl2N5
MW 352.26

Purity: 99%
Soluble in DMSO

SHP099

Description

Highly potent, selective and orally bioavailable SHP2 inhibitor (IC50 value 0.071 μM) that stabilizes SHP2 in an auto-inhibited conformation. SHP099 potently inhibits ERK phosphorylation and the growth of cancer cell lines that have alterations in RTKs or other tyrosine kinases such as the Janus kinases JAK1 and JAK2. SHP099 showed no detectable activity against a panel of 21 phosphatases and 66 kinases (including the closest homologue SHP1), and only had modest activity against 5HT₃ when profiled against a preclinical safety pharmacology panel representing 49 common adverse drug reaction targets.

J Garcia Fortanet et al. Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor. J Med Chem. 2016 Sep 8;59(17):7773-82.

YN Chen et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52.

Highly potent, selective and orally bioavailable SHP2 inhibitor

Chemical name

6-(4-amino-4-methylpiperidin-1-yl)-3-(2,3-dichlorophenyl)pyrazin-2-amine

Parent CAS No.

[1801747-42-1]

产品资料