| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S408002-1ml |
1ml |
现货  |
|
| 别名 | 苹果酸舒尼替尼(SU11248) |
|---|---|
| 英文别名 | (Z)-N-(2-(diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide ,(S)-2-hydroxysuccinic acid |
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Sunitinib (SU11248) malate |
| 生化机理 | 舒尼替尼（SU11248）苹果酸盐是一种多靶点 RTK 抑制剂，以血管内皮生长因子受体 2（Flk-1）和表皮生长因子受体β为靶点，在无细胞实验中的 IC50 值分别为 80 nM 和 2 nM，还能抑制 c-Kit。马来酸舒尼替尼能有效抑制 Ire1α 的自身磷酸化。马来酸舒尼替尼可增加死亡受体和线粒体依赖性凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 酪氨酸蛋白激酶受体 RET 抑制剂 |
| 产品介绍 |
Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.苹果酸舒尼替尼属于多靶点酪氨酸激酶抑制剂。 Information Sunitinib (SU11248) malate is a multi-targetedRTKinhibitor targetingVEGFR2 (Flk-1)andPDGFRβwithIC50of 80 nM and 2 nM in cell-free assays, and also inhibitsc-Kit. Sunitinib Malate effectively inhibits autophosphorylation ofIre1α. Sunitinib Malate increases 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 Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling 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. Sunitinib dosing at 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 ~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. cell lines： Concentrations：Dissolved in DMSO, final concentrations ~10 μM Incubation Time：24 and 48 hours Powder Purity:≥99% |
| IC50 | PDGFRβ, IC50: 2 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CCN(CC)CCNC(=O)C1=C(C)[NH]C(=C1C)/C=C/2C(=O)NC3=CC=C(F)C=C23.OC(CC(O)=O)C(O)=O |
| 分子量 | 532.56 |
| 溶解性 | Solubility (25°C) In vitro 4-Methylpyridine 100 mg/mL warmed with 50ºC Water: bath (401.13 mM); DMSO: 1 mg/mL warmed with 50ºC Water: bath (4.01 mM); Water: Insoluble; |
|---|
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Record the entire process by video | Conform |
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