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LY3200882

CAS号

1898283-02-7

分子式

C24H29N5O3

主要靶点

TGF-beta/Smad

仅限科研使用

Cat No : CM06628

Print datasheet

Synonyms

immune|inhibit|ATP-competitive|ALK5|anti-metastatic|Anti-cancer|phosphorylation|Inhibitor|LY 3200882|LY3200882|LY-3200882|TGF-beta|TGFbeta|TGF-b/Smad|TGFbeta/Smad|TGF-β/Smad|TGF-β Receptor|TGFβ|TGF-βRI (ALK5)|TGFβRI|TGFb|serine-threonine|Smad|SMAD|Transforming growth factor beta receptors

验证数据展示

  • CAS No.: 1898283-02-7

    LY3200882
    CAS#: 1898283-02-7

产品信息

CAS号 1898283-02-7
分子式 C24H29N5O3
主要靶点 TGF-beta/Smad
主要通路 干细胞
分子量 435.52
纯度 99.46%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 immune|inhibit|ATP-competitive|ALK5|anti-metastatic|Anti-cancer|phosphorylation|Inhibitor|LY 3200882|LY3200882|LY-3200882|TGF-beta|TGFbeta|TGF-b/Smad|TGFbeta/Smad|TGF-β/Smad|TGF-β Receptor|TGFβ|TGF-βRI (ALK5)|TGFβRI|TGFb|serine-threonine|Smad|SMAD|Transforming growth factor beta receptors

靶点活性

TGFβRI:38.2 nM (IC50)

体内活性

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].

体外活性

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 na?ve T cell activity and restore proliferation [1].

溶解度

DMSO:4.36 mg/mL (10 mM)

参考文献

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.

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