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抑制剂/激活剂

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凋亡与自噬

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Sunitinib 舒尼替尼; SU 11248

Sunitinib (SU 11248) 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 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。

货号：
TK0277
规格：

5mg

10mg

25mg

100mg
价格：
￥0.00

产品参数

CAS No.	557795-19-4
生物活性	Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
分子式	C22H27FN4O2
分子量	398.47
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 25 mg/mL (62.74 mM; Need ultrasonic and warming)
体内研究	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.
体外研究	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).
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纯度及产品资料	98%

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