LY3200882 - TGF-β Receptor 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELY3200882Cat. No.: HY-103021CAS No.: 1898283-02-7分式: CHNO分量: 435.52作靶点: TGF- Receptor作通路: TGF-beta/Smad储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 130 mg/mL (298.49 mM; Need ultrasonic

2、and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2961 mL 11.4805 mL 22.9611 mL5 mM 0.4592 mL 2.2961 mL 4.5922 mL10 mM 0.2296 mL 1.1481 mL 2.2961 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存

3、条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.74 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.74 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.74 mM)

4、; Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 LY3200882个新型且具有选择性的 TGF- 受体 1 型 (TGFRI) 抑制剂。IC50 & Target TGFRI 1体外研究 LY3200882 is a novel, highly selective inhibitor of TGF- receptor type 1 (TGFRI). LY3200882 potentlyinhibits TGF mediated SMAD phosphorylation

5、 in vitro in tumor and immune cells. LY3200882 has shownanti-metastatic activity in vitro in migration assays. In in vitro immune suppression assays, LY3200882 hasshown the ability to rescue TGF1 suppressed or T regulatory cell suppressed nave T cell activity andrestore proliferation 1.体内研究 LY320088

6、2 potently inhibits TGF mediated SMAD phosphorylation in vivo in subcutaneous tumors in adose dependent fashion. LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasistumor model (intravenous EMT6-LM2 model of triple negative breast cancer) 1.REFERENCES1. Huaxing Pei, et al. Abstract 955: LY3200882, a novel, highly selective TGFRI small molecule inhibitor. AACR; Cancer Res 2017;77(13Suppl):Abstract nr 955.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.