2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. Semaxinib

Semaxinib  (Synonyms: 司马沙尼; SU5416)

目录号: HY-10374 纯度: 99.96%
COA 产品使用指南

摩尔计算器

Semaxinib (SU5416) 是有效，选择性的 VEGFR (Flk-1/KDR) 抑制剂，IC50 为 1.23 μM。

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Semaxinib Chemical Structure

Semaxinib Chemical Structure

CAS No. : 204005-46-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥673
In-stock
5 mg ￥612
In-stock
10 mg ￥980
In-stock
50 mg ￥3000
In-stock
100 mg ￥5500
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Semaxinib:

Semaxinib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 42 篇科研文献

WB

    Semaxinib purchased from MCE. Usage Cited in: BMC Anesthesiol. 2019 Jul 9;19(1):127.  [Abstract]

    The hCMEC/D3 cells are incubated with TNF-α and VEGFR-2 inhibitor (SU5416, 10 μM). Left side shows the image of a representative Western blot for VEGF, p-VEGFR-2, p-ERK, ERK and occludin in hCMEC/D3 cells. Right side is the plot of normalized ratios of optical densities. β-actin is served as internal loading control.

    查看 VEGFR 亚型特异性产品:

    查看所有亚型
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Semaxinib (SU5416) is a potent and selective inhibitor of VEGFR (Flk-1/KDR) with an IC50 of 1.23 μM[1].

    IC50 & Target[1]

    Flk-1

    1.23 μM (IC50)

    体外研究
    (In Vitro)

    Semaxinib (SU5416) inhibits VEGF-driven mitogenesis in a dose-dependent manner with an IC50 of 0.04±0.02 μM (n=3). In contrast, Semaxinib (SU5416) blocks FGF-dependent mitogenesis of HUVECs with an IC50 of 50 μM (n=10). An IC50 of 20.26±5.2 μM, which is about 20-fold less in potency on PDGF-dependent autophosphorylation, is observed when SU5416 is tested in NIH 3T3 cells overexpressing the human PDGF receptor β[1].

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

    Semaxinib 相关抗体:
    体内研究
    (In Vivo)

    Daily administration of Semaxinib (SU5416) (i.p., 3 mg/kg/day) inhibits the local growth of C6 tumors in the colon. A comparable level of growth inhibition (62% by day 16; P=0.001) is observed for tumors growing in the colon in comparison with ones growing in the hindflank region (54% by day 18; P=0.001). These results indicate that Semaxinib (SU5416) could inhibit tumor growth at a site other than the subcutaneous implantation site, where the preexisting vasculature may be different[1]. Daily treatment with Semaxinib (SU5416) (25 mg/kg) results in a significantly lower tumor growth rate with tumor masses of up to 8% of that present in control animals by day 22 after implantation. Inhibition of tumor growth is clearly preceded by a marked reduction of the tissue area covered by the newly formed glioma microvasculature in the Semaxinib-treated group, indicating a reduced initial tumor vascularization[2].

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

    238.28

    Formula

    C15H14N2O
    CAS 号
    性状

    固体

    颜色

    Brown to orange

    中文名称

    司马沙尼
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMF 中的溶解度 : 50 mg/mL (209.84 mM; 超声助溶)

    DMSO 中的溶解度 : 10 mg/mL (41.97 mM; 超声助溶 (<60°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 4.1967 mL 20.9837 mL 41.9674 mL
    5 mM 0.8393 mL 4.1967 mL 8.3935 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。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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

    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： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (10.49 mM); 悬浊液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    • 方案 二

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

      Solubility: 2.25 mg/mL (9.44 mM); 悬浊液; 超声助溶

      此方案可获得 2.25 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例，取 100 μL 22.5 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。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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： 15% Solutol HS 15    10% Cremophor EL    35% PEG400    40% Water

      Solubility: 5 mg/mL (20.98 mM); 悬浊液; 超声助溶

    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

    只
    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）。
    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: 99.96%

    COA (291 KB) HNMR (207 KB) RP-HPLC (232 KB) LCMS (120 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay

    3T3Her2 and 488G2M2 are NIH3T3 fibroblast cell lines engineered to overexpress Her2 and to express human PDGF-BB and human PDGF receptor β. Both cell lines are cultured in DMEM supplemented with 2% CS and 2 mM L-glutamine. C6, Calu 6, A375, A431, and SF767T are plated in their respective growth medium at 2×103 cells/100 μL/well in 96-well, flat-bottomed plates. Semaxinib (SU5416) is serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture. Cell growth is measured after 96 h using the sulforhodamine B method. IC50s are calculated by curve fitting using four-parameter analysis[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][3]

    Mice[1]
    Female BALB/c nu/nu mice (20-22 g; 12 weeks of age) are used. Aseptic technique is used during this surgical procedure. A small midline incision (1 cm) is made in the abdomen directly over the colon. C6 cells are implanted (0.5×106 cells/animal) under the serosa of the colon using a 27-gauge needle. After implantation, all exposed sections of the intestine are returned into the abdominal cavity. The peritoneum and skin are closed using a 6.0 surgical suture and wound clips. The wound clips are removed 7 days after surgery. Animals are treated once daily with a 50 μL i.p. bolus injection of either Semaxinib (SU5416) or DMSO, beginning 1 day after implantation. Approximately 13-16 days after implantation, animals are euthanized, and local tumor growth on the colon is quantitated either by weighing the tumors or by measuring the tumors using venier calipers. Tumor volumes are calculated as the product of length×width×height.
    Rats[3]
    Male Sprague Dawley rats (n=60, 6-8 wk) are randomly divided among five groups: control (Con), Semaxinib (SU), pneumonectomy (PNx), Semaxinib+hypoxia (SuHx), and Semaxinib+PNx (SuPNx). The SuHx protocol is employed. Briefly, animals are injected with Semaxinib (25 mg/kg) dissolved in carboxymethylcellulose (CMC) and exposed to hypoxia (10%) for 4 wk followed by re-exposure to normoxia. PNx animals underwent a left pneumonectomy. Two days following PNx surgery an injection of Semaxinib is administered (25 mg/kg). The Con group received only the solvent CMC. Echocardiography is utilized at baseline (prehypoxia/presurgery), week 2, and week 6 to determine cardiac morphometry and function. Two and six weeks postsurgery/posthypoxia animals are anesthetized and right ventricle (RV) and left ventricle (LV) pressure measurements via catheterization are performed.

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

    Semaxinib 相关分类

    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。-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
    DMSO / DMF 1 mM 4.1967 mL 20.9837 mL 41.9674 mL 104.9186 mL
    5 mM 0.8393 mL 4.1967 mL 8.3935 mL 20.9837 mL
    10 mM 0.4197 mL 2.0984 mL 4.1967 mL 10.4919 mL
    15 mM 0.2798 mL 1.3989 mL 2.7978 mL 6.9946 mL
    20 mM 0.2098 mL 1.0492 mL 2.0984 mL 5.2459 mL
    25 mM 0.1679 mL 0.8393 mL 1.6787 mL 4.1967 mL
    30 mM 0.1399 mL 0.6995 mL 1.3989 mL 3.4973 mL
    40 mM 0.1049 mL 0.5246 mL 1.0492 mL 2.6230 mL
    DMF 50 mM 0.0839 mL 0.4197 mL 0.8393 mL 2.0984 mL
    60 mM 0.0699 mL 0.3497 mL 0.6995 mL 1.7486 mL
    80 mM 0.0525 mL 0.2623 mL 0.5246 mL 1.3115 mL
    100 mM 0.0420 mL 0.2098 mL 0.4197 mL 1.0492 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.

    Keywords:

    Semaxinib204005-46-9SU5416司马沙尼SU 5416SU-5416VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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