LY3200882 - TGF-β Receptor 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELY3200882Cat. No.: HY-103021CAS No.: 1898283-02-7分式: CHNO分量: 435.52作靶點(diǎn): TGF- Receptor作通路: TGF-beta/Smad儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 130 mg/mL (298.49 mM; Need ultrasonic

2、and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存

3、條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.74 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.74 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.74 mM)

4、; Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 LY3200882個(gè)新型且具有選擇性的 TGF- 受體 1 型 (TGFRI) 抑制劑。IC50 & Target TGFRI 1體外研究 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.體內(nèi)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.