Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor withIC₅₀s of 80 nM and 2 nM forVEGFR2andPDGFRβ, respectively^[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation ofIre1αby inhibiting autophosphorylation and consequent RNase activation^[2].

Sunitinib Malate is also a good inhibitor of KIT and FLT-3^[1]. In RS4;11 cells (FLT3-WT), treatment with Sunitinib (SU11248) inhibits FLT3-WT phosphorylation in a dose-dependent manner with IC₅₀of approximately 250 nM. In MV4;11 cells that express FLT3-ITD, Sunitinib inhibits FLT3-ITD phosphorylation in a dose-dependent manner with an IC₅₀of 50 nM following a 2-hour treatment^[3].In biochemical assays, Sunitinib (SU11248) exhibits competitive inhibition (with regard to ATP) against Flk-1 and PDGFRβ with K_ivalues of 9 nM and 8 nM, respectively. Sunitinib is also a competitive, albeit less potent, inhibitor of FGFR1 tyrosine kinase activity, with a K_ivalue 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 IC₅₀values 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)^[4].

Sunitinib Malate has very good oral bioavailability, is highly efficacious in a number of preclinical tumor models, and is well tolerated at efficacious doses^[1]. 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^[4].

398.47

Solid

C₂₂H₂₇FN₄O₂

557795-19-4

舒尼替尼；苏尼替尼

Room temperature in continental US; may vary elsewhere.

DMSO : 20.83 mg/mL(52.27 mM;ultrasonic and warming and heat to 80℃)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 1.11 mg/mL (2.79 mM); Clear solution

  此方案可获得 ≥ 1.11 mg/mL (2.79 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 11.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 1.11 mg/mL (2.79 mM); Clear solution

  此方案可获得 ≥ 1.11 mg/mL (2.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 11.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。