LXS196 - PKC 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELXS196Cat. No.: HY-101569CAS No.: 1874276-76-2分式: CHFNO分量: 472.47作靶点: PKC作通路: Epigenetics; 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 : 100 mg/mL (211.65 mM)* means soluble,

2、 but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1165 mL 10.5827 mL 21.1654 mL5 mM 0.4233 mL 2.1165 mL 4.2331 mL10 mM 0.2117 mL 1.0583 mL 2.1165 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

3、清的储备液可以根据储存条件，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 (5.29 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 (5.29 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small

4、Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.29 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 LXS196有效的、选择性的和具有服活性的蛋激酶C (PKC) 抑制剂，对PKC、PKC 和 GSK3 的 IC50值分别为 1.9 nM、0.4 nM 和 3.1 M。可于治疗葡萄膜素瘤。IC50 & Target PKC PKC GSK31.9 nM (IC50) 0.4 nM (IC50) 3.1 M (IC50)体外研究 Upon oral administration, protein k

5、inase C inhibitor LXS196 binds to and inhibits PKC, which prevents theactivation of PKC-mediated signaling pathways. This may lead to the induction of cell cycle arrest andapoptosis in susceptible tumor cells. PKC, a serine/threonine protein kinase overexpressed in certain typesof cancer cells, is i

6、nvolved in tumor cell differentiation, proliferation, invasion and survival 1.体内研究 LXS196 (compound 9) (15, 30, 75, 150 mg/kg, P.O., mice) shows improved efficacy (regression) in a 92.1GNAQ uveal melanoma xenograft model in a dose-dependently manner 2.Animal Model: Mice implanted with 92.1 GNAQ muta

7、nt uveal melanoma cells 2.Dosage: 15, 30, 75, 150 mg/kgAdministration: P.O. (bid) for 35 daysResult: Dose-dependently suppressed the tumor growth.REFERENCES1. Protein Kinase C Inhibitor LXS1962. US20180179181.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use o