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

Sunitinib Malate  (Synonyms: 苹果酸舒尼替尼; SU 11248 Malate)

目录号: HY-10255 纯度: 99.91%
COA 产品使用指南

Sunitinib Malate (SU 11248 Malate) 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 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。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Sunitinib Malate Chemical Structure

Sunitinib Malate Chemical Structure

CAS No. : 341031-54-7

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥715
In-stock
100 mg ¥650
In-stock
200 mg ¥950
In-stock
500 mg ¥1500
In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Sunitinib Malate:

MCE 顾客使用本产品发表的 49 篇科研文献

WB
RT-PCR
IHC
Cell Viability Assay
IF

    Sunitinib Malate 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 Malate 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 Malate 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 Malate 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 Malate 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 Malate 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 Malate 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 Malate 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 Malate 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 Malate 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 Malate 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).

    Sunitinib Malate 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).

    查看 PDGFR 亚型特异性产品:

    查看 VEGFR 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 Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

    IC50 & Target[1]

    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

    532.56

    Formula

    C26H33FN4O7

    CAS 号
    性状

    固体

    颜色

    Light yellow to khaki

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : ≥ 15 mg/mL (28.17 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 12.5 mg/mL (23.47 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈3))

    H2O 中的溶解度 : 3.33 mg/mL (6.25 mM; 超声助溶 (<60°C))

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.8777 mL 9.3886 mL 18.7772 mL
    5 mM 0.3755 mL 1.8777 mL 3.7554 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, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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

    动物实验:

    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: 100 mM Citrate buffer 中最大溶解度

      Solubility: 10 mg/mL (18.78 mM); 悬浊液; Need ultrasonic and adjust pH to 5 with HCl

    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (4.69 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 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。
    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, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    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: 99.91%

    参考文献
    Kinase Assay
    [2]

    Biochemical assays to determine the activity of Sunitinib against different protein kinases are performed. Ki values for SU11248 against Flk-1, PDGFRβ, and FGFR1 are determined using glutathione S-transferase-fusion proteins containing the complete cytoplasmic domain of the RTK. Cellular assays to directly determine the ability of SU11248 to inhibit ligand-dependent RTK phosphorylation or cell proliferation and mitogenic responses are performed using serum-starved cells stimulated with 40 ng/mL VEGF165 (Flk-1/KDR), 0.5 μg/mL basic FGF (FGFR), or 50 ng/mL PDGF-AA (PDGFRα) or PDGF-BB (PDGFRβ)[2].

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

    Cell Assay
    [3]

    RS4;11 and MV4;11 cell lines are starved overnight in medium containing 0.1% FBS prior to addition of SU11248 (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 g) 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 SU11248 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]
    Forty female Sprague-Dawley rats (200-230 g) are used. Each group consists of 5-10 animals fed ad libitum. 1×104 Walker 256 cells are injected into the left abdominal mammary fat pad, under gas anesthesia (2% isoflurane). Rats are weighed daily and given Sunitinib malate (30 mg/kg) and/or Fingolimod (5 mg/kg) in olive oil by gavage. The tumors are measured with calipers. The animals are anesthetized and killed by an intracardiac injection of ketamine (50 mg/mL) before tumor ulceration. Rats are dissected to detect pulmonary, liver, kidney, or intestinal metastasis.

    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, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / H2O / DMSO 1 mM 1.8777 mL 9.3886 mL 18.7772 mL 46.9431 mL
    5 mM 0.3755 mL 1.8777 mL 3.7554 mL 9.3886 mL
    H2O / DMSO 10 mM 0.1878 mL 0.9389 mL 1.8777 mL 4.6943 mL
    15 mM 0.1252 mL 0.6259 mL 1.2518 mL 3.1295 mL
    20 mM 0.0939 mL 0.4694 mL 0.9389 mL 2.3472 mL
    DMSO 25 mM 0.0751 mL 0.3755 mL 0.7511 mL 1.8777 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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.

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称:

     

    * 需求量:

    * 客户姓名:

     

    * Email:

    * 电话:

     

    * 公司或机构名称:

       留言给我们:

    Bulk Inquiry

    Inquiry Information

    产品名称:
    Sunitinib Malate
    目录号:
    HY-10255
    需求量: