N-Desethyl Sunitinib-d5N-去乙基-舒

N-Desethyl Sunitinib-d5 hydrochloride 产品活性：N-Desethyl Sunitinib-d5 (hydrochloride)是氘代标记的N-Desethyl Sunitinib。N-Desethyl Sunitinib (SU-12662) 是 Sunitinib 的代谢物。Sunitinib是有效的，ATP 竞争的 VEGFR，PDGFRβ 和 KIT 抑制剂，能够抑制 VEGFR -1，VEGFR -2，VEGFR -3，PDGFRβ 和 KIT 的活性，Ki 值分别为 2，9，17，8 和 4 nM。 产品来源： www.medchemexpress.cn/n-desethyl-sunitinib-d5-hydrochloride.html 研究领域：Others | Metabolic Enzyme/Protease 作用靶点：Isotope-Labeled Compounds | Drug Metabolite In Vitro: Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.Sunitinib also potently inhibits Kit and FLT-3. Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. In Vivo: Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo. Sunitinib (80 mg/kg/day) for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with appr 40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size.?Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. 相关产品：Clozapine N-oxide | SN-38 | Calcitriol | Urolithin A | Oseltamivir acid | Teriflunomide | Phosphoramide mustard cyclohexanamine | Gemfibrozil 1-O-β-glucuronide | 5-Fluorouridine | Trimethylamine N-oxide | 4-Hydroperoxy cyclophosphamide | Mycophenolate Mofetil | Monomethyl fumarate | VRT-043198 | Penicillamine | Linsidomine hydrochloride | GS-443902 trisodium | MTIC | Desloratadine | Pyocyanin | Nortriptyline hydrochloride | Paraxanthine | 4-Hydroxymephenytoin | L-Lactic acid-13C3 sodium | Homovanillic acid | L-Valine-d8 | Ercalcitriol | Paliperidone | Abemaciclib metabolite M2 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种TOP期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪前沿的制药及生命科学研究进展，为您提供全球前沿的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。