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SC-43
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SC-43图片
CAS NO:1400989-25-4
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议

产品介绍
SC-43 是一种具有口服活性的SHP-1 (PTPN6)激动剂。它是SoRafenib 的衍生物,可抑制STAT3的磷酸化并诱导细胞凋亡,具有抗纤维化和抗癌作用。

产品描述

SC-43 is a potent and orally active agonist of SHP-1 (PTPN6). SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis, and with anti-fibrotic and anticancer effects.

体外活性

SC-43, a sorafenib derivative.SC-43-induced apoptosis in cholangiocarcinoma (CCA) via a novel mechanism.?Three CCA cell lines (HuCCT-1, KKU-100 and CGCCA) were treated with SC-43 to determine their sensitivity to SC-43-induced cell death and apoptosis.?SC-43 activated SH2 domain-containing phosphatase 1 (SHP-1) activity, leading to p-STAT3 and downstream cyclin B1 and Cdc2 downregulation, which induced G2-M arrest and apoptotic cell death.?Importantly, SC-43 augmented SHP-1 activity by direct binding to N-SH2 and relief of its autoinhibition.?Deletion of the N-SH2 domain (dN1) or point mutation (D61A) of SHP-1 counteracted the effect of SC-43-induced SHP-1 phosphatase activation and antiproliferation ability in CCA cells[1].

体内活性

In vivo assay revealed that SC-43 exhibited xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation[1].

Cas No.

1400989-25-4

分子式

C21H13ClF3N3O2

分子量

431.8

储存和溶解度

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years