SU14813马来酸盐
基本信息
产品名称：
SU14813马来酸盐
英文名称：
SU14813 maleate
国产/进口：
进口
产地/品牌：
美国/TargetMol
型号：
参考报价：
面议
销售商：
总点击数：
112
更新日期：
2026-04-01
产品类别：
性能参数
Product Introduction
Bioactivity
英文名: SU14813 maleate
描述: SU14813 maleate is an inhibitor of multi-targeted receptor tyrosine kinases (IC50s: 2, 50, 4, 15 nM for VEGFR1, VEGFR2, PDGFRβ, and KIT).
细胞实验: Passages 4 to 5 human umbilical vein endothelial cells are grown to subconfluency in EGM2 medium containing 10% FBS, endothelial cell growth supplement, and 10 μg/mL sodium heparin. The cells are seeded in 96-well plates at 10,000 per well in F12K medium and 10% FBS. The next day, cells are starved for 18 hours in F12K+1% FBS and then incubated with SU14813 in various concentrations. 45 minutes later, 20 ng/mL growth factor [VEGF or basic fibroblast growth factor (bFGF)] is introduced into the assay. Three days later, cell numbers are determined using the MTT assay.
动物实验: SU14813 is evaluated for its efficacy and synergism in combination with the microtubule inhibitor docetaxel in docetaxel-resistant murine LLC model. SU14813 is administered p.o. twice daily (BID) at doses of 10, 40, 80, or 120 mg/kg beginning on day 5 after tumor implantation. Docetaxel 40 mg/kg (mouse maximum tolerated dose) is administered i.v. thrice-weekly also beginning on day 5 after tumor implantation.
体外活性: SU14813 inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells), PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC50 values of 5.2, 9.9, and 11.2 nM, respectively. SU14813 inhibits the growth of U-118MG (IC50: 50-100 nM).
体内活性: SU14813 inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion. The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200 ng/mL. Used as monotherapy, SU14813 exhibits broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduced growth of various established xenografts derived from human or rat tumor cell lines.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 100 mg/mL (179.03 mM)
关键字: SU-14813 maleate | SU14813 maleate | SU 14813 Maleate | SU-14813 Maleate | SU14813 Maleate
相关产品: Vorolanib | Regorafenib monohydrate | Compound Lup-20(29)-en-3-yl acetate | Telatinib | AKB-6899 | Brolucizumab | Riddelline | AG 1406 | Sorafenib-d3 | Pz-1
Bioactivity
英文名: SU14813 maleate
描述: SU14813 maleate is an inhibitor of multi-targeted receptor tyrosine kinases (IC50s: 2, 50, 4, 15 nM for VEGFR1, VEGFR2, PDGFRβ, and KIT).
细胞实验: Passages 4 to 5 human umbilical vein endothelial cells are grown to subconfluency in EGM2 medium containing 10% FBS, endothelial cell growth supplement, and 10 μg/mL sodium heparin. The cells are seeded in 96-well plates at 10,000 per well in F12K medium and 10% FBS. The next day, cells are starved for 18 hours in F12K+1% FBS and then incubated with SU14813 in various concentrations. 45 minutes later, 20 ng/mL growth factor [VEGF or basic fibroblast growth factor (bFGF)] is introduced into the assay. Three days later, cell numbers are determined using the MTT assay.
动物实验: SU14813 is evaluated for its efficacy and synergism in combination with the microtubule inhibitor docetaxel in docetaxel-resistant murine LLC model. SU14813 is administered p.o. twice daily (BID) at doses of 10, 40, 80, or 120 mg/kg beginning on day 5 after tumor implantation. Docetaxel 40 mg/kg (mouse maximum tolerated dose) is administered i.v. thrice-weekly also beginning on day 5 after tumor implantation.
体外活性: SU14813 inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells), PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC50 values of 5.2, 9.9, and 11.2 nM, respectively. SU14813 inhibits the growth of U-118MG (IC50: 50-100 nM).
体内活性: SU14813 inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion. The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200 ng/mL. Used as monotherapy, SU14813 exhibits broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduced growth of various established xenografts derived from human or rat tumor cell lines.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 100 mg/mL (179.03 mM)
关键字: SU-14813 maleate | SU14813 maleate | SU 14813 Maleate | SU-14813 Maleate | SU14813 Maleate
相关产品: Vorolanib | Regorafenib monohydrate | Compound Lup-20(29)-en-3-yl acetate | Telatinib | AKB-6899 | Brolucizumab | Riddelline | AG 1406 | Sorafenib-d3 | Pz-1
公司简介
TargetMol（陶术）作为一家全球性的生物医药领域高科技企业，我们致力于为高校、研究所、医院、企业等各类生物医药研发机构提供优质的产品和服务，为全球医药科学家更高效地完成科研工作助力。可提供20,000+种 抑制剂和激动剂 、800+种 化合物库 、19,000+种 天然产物 ，以及9,000+种 重组蛋白 、多种 多肽 、抗体 和 生命科学试剂盒 等。此外，在上海，TargetMol研发中心配备了 CADD & AIDD研究中心、药理实验室和药物化学合成 平台三大技术中心，可提供虚拟筛选、化合物活性测试、分子间结合力检测和化合物结构优化等技术服务，多方位满足用户的研发需求。
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