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CAS No. : 341031-54-7
MCE 国际站:Sunitinib Malate
产品活性:Sunitinib Malate (SU 11248 Malate) 是一种多靶点受体酪氨酸激酶抑制剂,抑制 VEGFR2 和 PDGFRβ 的 IC50 分别为80 nM 和 2 nM。Sunitinib Malate 是ATP 竞争性抑制剂,可通过抑制自身磷酸化和随后的 RNase 激活来有效抑制 Ire1α 的磷酸化。
研究领域:Protein Tyrosine Kinase/RTK | Cell Cycle/DNA Damage | Autophagy | Apoptosis
作用靶点:PDGFR | VEGFR | IRE1 | Mitophagy | Autophagy | Apoptosis
In Vitro: Sunitinib Malate is also a good inhibitor of KIT and FLT-3. In RS4;11 cells (FLT3-WT), treatment with Sunitinib (SU11248) inhibits FLT3-WT phosphorylation in a dose-dependent manner with IC50 of approximately 250 nM. In MV4;11 cells that express FLT3-ITD, Sunitinib inhibits FLT3-ITD phosphorylation in a dose-dependent manner with an IC50 of 50 nM following a 2-hour treatment.In biochemical assays, Sunitinib (SU11248) exhibits competitive inhibition (with regard to ATP) against Flk-1 and PDGFRβ with Ki values of 9 nM and 8 nM, respectively. Sunitinib is also a competitive, albeit less potent, inhibitor of FGFR1 tyrosine kinase activity, with a Ki value of 0.83 μM. In addition to these three structurally related split kinase domain RTKs, the activity of Sunitinib has also been evaluated against a broad panel of additional tyrosine and serine/threonine kinases. In these biochemical assays, the IC50 values for Sunitinib are generally at least 10-fold higher than those for Flk-1 and PDGFR (e.g., IC50values of: >10 μM for EGFR and Cdk2; 4 μM for Met; 2.4 μM for IGFR-1; 0.8 μM for Abl; and 0.6 μM for Src).
In Vivo: Sunitinib Malate has very good oral bioavailability, is highly efficacious in a number of preclinical tumor models, and is well tolerated at efficacious doses. Sunitinib (80 mg/kg/day) inhibits the growth of established SF763T and Colo205 tumor xenografts in athymic mice. Sunitinib (SU11248) treatment effectively inhibits the growth of established tumor xenografts.
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