Taladegib-LY2940680-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETaladegibCat. No.: HY-13242CAS No.: 1258861-20-9Synonyms: LY2940680分式: CHFNO分量: 512.5作靶点: Smo作通路: Stem Cell/Wnt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 : 50 mg/mL (97.56 mM; Need ultra

2、sonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9512 mL 9.7561 mL 19.5122 mL5 mM 0.3902 mL 1.9512 mL 3.9024 mL10 mM 0.1951 mL 0.9756 mL 1.9512 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条件，适当保存；

3、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 (4.88 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 (4.88 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的抑制剂师ww

4、w.MedChemESolubility: 2.5 mg/mL (4.88 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Taladegib (LY2940680)种 smoothened 受体拮抗剂。IC50 & Target Smo 1体外研究 Taladegib, a small-molecule antagonist of the smoothened receptor, shows a slight inhibitory effect on cellproliferation without differences between mucin-

5、(IC50: Taladegib=49.84.5 M) and mixed-Cholangiocarcinoma (CCA) (IC50: Taladegib=61.221.1 M) 1. The IC50 for Taladegib inhibition of3HMRT-92 binding is right shifted (3- to 100-fold) for the S387AECL2, L325F3.36f, and D473H6.54fmutants but did not differ from that of WT receptor for the other mutants

6、. The ability of SANT-1 to inhibit3HMRT-92 binding to V329F3.40f and T466F6.47f mutants is abolished, and it is severely impaired forL325F3.40f, I408F5.51f, and M525G7.45f mutants (4- to 140-fold drop of the IC50), but is not modified for theS387AECL2 mutant. Taken together, these data confirm our d

7、ocking hypothesis that MRT-92-binding modediffers from that of either Taladegib or SANT-1 by simultaneously occupying binding sites 1 and 2 2.户使本产品发表的科研献 J Genet Genomics. 2018 May 20;45(5):237-246.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Fraveto A, et al, Sensitivity of

8、 Human Intrahepatic Cholangiocarcinoma Subtypes to Chemotherapeutics and Molecular Targeted Agents:A Study on Primary Cell Cultures. PLoS One. 2015 Nov 16;10(11):e0142124.2. Hoch L, et al. MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of theSmoo

9、thened receptor. FASEB J. 2015 May;29(5):1817-29.3. Ma W, et al. Reduced Smoothened level rescued A-induced memory deficits and neuronal inflammation in animal models ofAlzheimers disease. J Genet Genomics. 2018 May 20;45(5):237-246.McePdfHeightCaution: Product has not been fully validated for medical