1. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage Autophagy Apoptosis
  2. VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis
  3. Sunitinib

Sunitinib  (Synonyms: 舒尼替尼; SU 11248)

目录号: HY-10255A 纯度: 98.96%
COA 产品使用指南

Sunitinib (SU 11248) 是一种多靶点受体酪氨酸激酶抑制剂,抑制 VEGFR2PDGFRβIC50 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。

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Sunitinib Chemical Structure

Sunitinib Chemical Structure

CAS No. : 557795-19-4

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     可免费申领三个不同产品的试用装。

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200 mg ¥950
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500 mg ¥1500
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 43 篇科研文献

WB
RT-PCR
IHC
Cell Viability Assay
IF

    Sunitinib purchased from MCE. Usage Cited in: J Pharm Anal. 2023 Apr 19.

    Sunitinib (3 μM; 24 h) increases the expression of γ-H2Ax and Temozolomide (TMZ; 10 μM; 24 h) increases the induction of Sunitinib, in T98G cells.

    Sunitinib purchased from MCE. Usage Cited in: J Pharm Anal. 2023 Apr 19.

    Sunitinib (3 μM; 24 h) increases the expression of γ-H2Ax and Temozolomide (TMZ; 10 μM; 24 h) increases the induction of Sunitinib, in T98G cells.

    Sunitinib purchased from MCE. Usage Cited in: J Pharm Anal. 2023 Apr 19.

    Sunitinib (0-100 μM; 72 h) induces significant cell death in T98G cells.

    Sunitinib purchased from MCE. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefinitib at 2.5 µM, Sunitinib at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

    Sunitinib purchased from MCE. Usage Cited in: EBioMedicine. 2018 Nov;37:344-355.  [Abstract]

    Sutent (Sunitinib Malate) treatment decreases lipid accumulation in adipose and liver tissues and increases UCP1 expression in brown adipose tissue. Representative images of immunohistochemistry stainining of UCP1 in BAT.

    Sunitinib purchased from MCE. Usage Cited in: EBioMedicine. 2018 Nov;37:344-355.  [Abstract]

    Sutent (Sunitinib Malate) treatment decreases lipid accumulation in adipose and liver tissues and increases UCP1 expression in brown adipose tissue. Western blot analysis of UCP1 protein expression level in mouse brown adipose.

    Sunitinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134.  [Abstract]

    Abemaciclib causes increased PARP cleavage in RCC. In Caki-1 cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with Sunitinib.

    Sunitinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134.  [Abstract]

    Abemaciclib causes increased PARP cleavage in RCC. In 786-O cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with Sunitinib.

    Sunitinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 15;8(67):111110-111118.  [Abstract]

    In cell EC50 determination of CHMFL-KIT-031 with parental Colo320DM (KIT wt) and KIT V559D overexpressed Colo320DM cells.

    Sunitinib purchased from MCE. Usage Cited in: J Med Chem. 2016 Sep 22;59(18):8456-72.  [Abstract]

    Effect of compounds 1 (Imatinib), 2 (Sunitinib), and 35 on cKIT mediated signaling pathways in GIST-T1 and GIST-5R cancer cell lines.

    Sunitinib purchased from MCE. Usage Cited in: Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81.  [Abstract]

    The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/Sunitinib (2 uM, 3 uM) significantly decreases expression of MEK1 and its phosphorylated protein (p-MEK1/2, p-ERK1/2) as assayed by Western blot (with GAPDH as internal control).

    Sunitinib purchased from MCE. Usage Cited in: Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81.  [Abstract]

    The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/Sunitinib (2 uM, 3 uM) significantly decreases expression of MEK1 and its phosphorylated protein (p-MEK1/2, p-ERK1/2) as assayed by RT-PCR (with β-actin as internal control).

    查看 VEGFR 亚型特异性产品:

    查看 PDGFR 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    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[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

    IC50 & Target

    VEGFR2

    80 nM (IC50)

    PDGFRβ

    2 nM (IC50)

    体外研究
    (In Vitro)

    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 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[3].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)[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (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[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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    398.47

    Formula

    C22H27FN4O2

    CAS 号
    性状

    固体

    颜色

    Yellow to orange

    中文名称

    舒尼替尼;苏尼替尼

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 20.83 mg/mL (52.27 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5096 mL 12.5480 mL 25.0960 mL
    5 mM 0.5019 mL 2.5096 mL 5.0192 mL
    查看完整储备液配制表

    * 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°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    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

    • 方案 一

      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); 澄清溶液

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

      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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 1.11 mg/mL (2.79 mM); 澄清溶液

      此方案可获得 ≥ 1.11 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      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。

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 98.96%

    参考文献
    Cell Assay
    [3]

    RS4;11 and MV4;11 cell lines are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib (1 nM, 5 nM, 10 nM, 25 nM, 75 nM, 100 nM, 250 nM, 500 nM) and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay in triplicate for each condition, as described by the manufacturer. Trypan blue cell viability assays are performed in parallel and yielded similar results[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][4]

    Mice[2]
    Female nu/nu mice (8-12 weeks old, 25 grams) are used. Briefly, 3-5×106 tumor cells are implanted s.c. into the hind flank region of mice on day 0. Daily treatment of tumor-bearing mice with oral administration of Sunitinib as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution is initiated once the tumors reached the indicated average size. Tumor growth is evaluated based on twice-weekly measurement of tumor volume. Typically, studies are terminated when tumors in vehicle-treated animals reach an average size of 1000 mm3 or when the tumors are judged to adversely effect the well being of the animals.
    Rats[4]
    Adult male Wistar rats (325-349 g) are used. To validate the ability of the time-lapse imaging method to evaluate the anti-angiogenic effects for a given drug treatment, two drug studies are conducted. In the first study, mesenteric windows are harvested from adult male Wistar rats and cultured for 3 days according to the two experimental groups: 1) 10% serum (n=8 tissues from 4 rats), and 2) 10% serum+Sunitinib (5 μM; n=8 tissues from 4 rats).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 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°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5096 mL 12.5480 mL 25.0960 mL 62.7400 mL
    5 mM 0.5019 mL 2.5096 mL 5.0192 mL 12.5480 mL
    10 mM 0.2510 mL 1.2548 mL 2.5096 mL 6.2740 mL
    15 mM 0.1673 mL 0.8365 mL 1.6731 mL 4.1827 mL
    20 mM 0.1255 mL 0.6274 mL 1.2548 mL 3.1370 mL
    25 mM 0.1004 mL 0.5019 mL 1.0038 mL 2.5096 mL
    30 mM 0.0837 mL 0.4183 mL 0.8365 mL 2.0913 mL
    40 mM 0.0627 mL 0.3137 mL 0.6274 mL 1.5685 mL
    50 mM 0.0502 mL 0.2510 mL 0.5019 mL 1.2548 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    Sunitinib
    目录号:
    HY-10255A
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