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LY3200882
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。
LY3200882图片
CAS NO:1898283-02-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
LY3200882 是一种有效的、高选择性、ATP 竞争性和口服活性的 TGF-β 受体 1 型 (ALK5) 抑制剂,IC50 为 38.2 nM。
Cas No.1898283-02-7
Canonical SMILESOC(C)(C)C1=NC=CC(NC2=NC=CC(OC3=CN(C4CC4)N=C3C5CCOCC5)=C2)=C1
分子式C24H29N5O3
分子量435.52
溶解度DMSO : 130 mg/mL (298.49 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).

LY3200882 is a novel, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells. LY3200882 has shown anti-metastatic activity in vitro in migration assays. In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naive T cell activity and restore proliferation[1].

LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose dependent fashion. LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer)[1].

References:
[1]. Huaxing Pei, et al. Abstract 955: LY3200882, a novel, highly selective TGFβRI small molecule inhibitor. AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 955.