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Sunitinib Malate
点击次数：303发布时间：2013/4/3 11:19:16
更新日期：2022/8/19 17:45:40
所 在 地：美洲
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详细内容
Sunitinib Malate
上海义森生物科技有限公司
技术数据:
分子量（MW）: 532.56 
化学式: C22H27FN4O2.C4H6O5
溶解度: DMSO 15mg/mL Water <1mg/mL Ethanol <1mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 341031-54-7, 557795-19-4 （free base）, 1126641-10-8 （ Maleic acid）
生物活性
Sunitinib （Sutent） is a multitargeted FLT3, PDGFRs, VEGFRs, ａnd Kit kinase inhibitor with Ki of 0.009 ａnd 0.008 µM for Flk-1 ａnd PDGFR, respectively. In RS4;11 cells （FLT3-WT）, addition of FL was necessary to stimulate FLT3 phosphorylation, ａnd treatment with SU11248 inhibited FLT3-WT phosphorylation in a dose-dependent manner with a 50% inhibitory concentration of approximately 250 nM. In MV4;11 cells that express FLT3-ITD, it is noteworthy that both high ａnd low molecular weight forms of FLT3 are phosphorylated in the absence of FLT3 ligand （FL）, consistent with expression of FLT3-ITD. Sunitinib Malate （Sutent, SU11248） inhibited FLT3-ITD phosphorylation in a dose-dependent manner with an IC50 of 50 nM following a 2-hour treatment. Evaluating the ability of Sunitinib （Sutent） to inhibit ligand-dependent receptor phosphorylation in cells, the effect of sunitinib （Sutent） on ligand-dependent proliferation of cells was examined. Sunitinib （Sutent） inhibited VEGF- ａnd FGF-induced proliferation of HUVECs with IC50 of 0.04 ａnd 0.7 µM, respectively. Sunitinib （Sutent） also inhibited PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRα or PDGFRβ with IC50 of 0.03 ａnd 0.07 µM, respectively. [1][2]
技术数据:
分子量（MW）: 532.56 化学式: C22H27FN4O2.C4H6O5
溶解度: DMSO 15mg/mL Water <1mg/mL Ethanol <1mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 341031-54-7, 557795-19-4 （free base）, 1126641-10-8 （ Maleic acid）
生物活性
Sunitinib （Sutent） is a multitargeted FLT3, PDGFRs, VEGFRs, ａnd Kit kinase inhibitor with Ki of 0.009 ａnd 0.008 µM for Flk-1 ａnd PDGFR, respectively. In RS4;11 cells （FLT3-WT）, addition of FL was necessary to stimulate FLT3 phosphorylation, ａnd treatment with SU11248 inhibited FLT3-WT phosphorylation in a dose-dependent manner with a 50% inhibitory concentration of approximately 250 nM. In MV4;11 cells that express FLT3-ITD, it is noteworthy that both high ａnd low molecular weight forms of FLT3 are phosphorylated in the absence of FLT3 ligand （FL）, consistent with expression of FLT3-ITD. Sunitinib Malate （Sutent, SU11248） inhibited FLT3-ITD phosphorylation in a dose-dependent manner with an IC50 of 50 nM following a 2-hour treatment. Evaluating the ability of Sunitinib （Sutent） to inhibit ligand-dependent receptor phosphorylation in cells, the effect of sunitinib （Sutent） on ligand-dependent proliferation of cells was examined. Sunitinib （Sutent） inhibited VEGF- ａnd FGF-induced proliferation of HUVECs with IC50 of 0.04 ａnd 0.7 µM, respectively. Sunitinib （Sutent） also inhibited PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRα or PDGFRβ with IC50 of 0.03 ａnd 0.07 µM, respectively. [1][2]
技术数据:
分子量（MW）: 532.56 化学式: C22H27FN4O2.C4H6O5
溶解度: DMSO 15mg/mL Water <1mg/mL Ethanol <1mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 341031-54-7, 557795-19-4 （free base）, 1126641-10-8 （ Maleic acid）
生物活性
Sunitinib （Sutent） is a multitargeted FLT3, PDGFRs, VEGFRs, ａnd Kit kinase inhibitor with Ki of 0.009 ａnd 0.008 µM for Flk-1 ａnd PDGFR, respectively. In RS4;11 cells （FLT3-WT）, addition of FL was necessary to stimulate FLT3 phosphorylation, ａnd treatment with SU11248 inhibited FLT3-WT phosphorylation in a dose-dependent manner with a 50% inhibitory concentration of approximately 250 nM. In MV4;11 cells that express FLT3-ITD, it is noteworthy that both high ａnd low molecular weight forms of FLT3 are phosphorylated in the absence of FLT3 ligand （FL）, consistent with expression of FLT3-ITD. Sunitinib Malate （Sutent, SU11248） inhibited FLT3-ITD phosphorylation in a dose-dependent manner with an IC50 of 50 nM following a 2-hour treatment. Evaluating the ability of Sunitinib （Sutent） to inhibit ligand-dependent receptor phosphorylation in cells, the effect of sunitinib （Sutent） on ligand-dependent proliferation of cells was examined. Sunitinib （Sutent） inhibited VEGF- ａnd FGF-induced proliferation of HUVECs with IC50 of 0.04 ａnd 0.7 µM, respectively. Sunitinib （Sutent） also inhibited PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRα or PDGFRβ with IC50 of 0.03 ａnd 0.07 µM, respectively. [1][2]
技术数据:
| 分子量（MW）: | 532.56 | |
|---|---|---|
| 化学式: | C22H27FN4O2.C4H6O5 | |
| 溶解度: | DMSO 15mg/mL Water <1mg/mL Ethanol <1mg/mL | |
| 纯度: | >99% | |
| 稳定性: | at -20℃ 2 years | |
| CAS号: | 341031-54-7, 557795-19-4 （free base）, 1126641-10-8 （ Maleic acid） |
生物活性
Sunitinib （Sutent） is a multitargeted FLT3, PDGFRs, VEGFRs, ａnd Kit kinase inhibitor with Ki of 0.009 ａnd 0.008 µM for Flk-1 ａnd PDGFR, respectively. In RS4;11 cells （FLT3-WT）, addition of FL was necessary to stimulate FLT3 phosphorylation, ａnd treatment with SU11248 inhibited FLT3-WT phosphorylation in a dose-dependent manner with a 50% inhibitory concentration of approximately 250 nM. In MV4;11 cells that express FLT3-ITD, it is noteworthy that both high ａnd low molecular weight forms of FLT3 are phosphorylated in the absence of FLT3 ligand （FL）, consistent with expression of FLT3-ITD. Sunitinib Malate （Sutent, SU11248） inhibited FLT3-ITD phosphorylation in a dose-dependent manner with an IC50 of 50 nM following a 2-hour treatment. Evaluating the ability of Sunitinib （Sutent） to inhibit ligand-dependent receptor phosphorylation in cells, the effect of sunitinib （Sutent） on ligand-dependent proliferation of cells was examined. Sunitinib （Sutent） inhibited VEGF- ａnd FGF-induced proliferation of HUVECs with IC50 of 0.04 ａnd 0.7 µM, respectively. Sunitinib （Sutent） also inhibited PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRα or PDGFRβ with IC50 of 0.03 ａnd 0.07 µM, respectively. [1][2]
