2. Protein Tyrosine Kinase/RTK
  3. RET FLT3 VEGFR c-Kit Bcr-Abl
  4. AST 487

AST 487  (Synonyms: NVP-AST 487)

目录号: HY-15002 纯度: 99.42%
COA 产品使用指南

摩尔计算器

AST 487 是一种 RET 激酶抑制剂，IC50 为 880 nM，抑制 RET 自磷酸化，及下游效应器激活，也抑制 Flt-3，IC50 为 520 nM。

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AST 487 Chemical Structure

AST 487 Chemical Structure

CAS No. : 630124-46-8

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     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 ￥1050
In-stock
1 mg ￥360
In-stock
5 mg ￥900
In-stock
10 mg ￥1500
In-stock
25 mg ￥2413
In-stock
50 mg ￥4500
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

AST 487 相关抗体

Top Publications Citing Use of Products

    AST 487 purchased from MCE. Usage Cited in: Cell Res. 2017 Dec;27(12):1441-1465.  [Abstract]

    AST487 effectively lowers mHTT levels, and this effect is mitigated by knocking down HIPK3, confirming that AST487 reduces mHTT levels via inhibiting HIPK3.

    查看 VEGFR 亚型特异性产品:

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    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

    AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.

    IC50 & Target

    IC50: 880 nM (RET), 170 nM (KDR), 790 nM (Flt-4), 500 nM (c-Kit), 520 nM (Flt-3), 20 nM (Abl)[1]
    体外研究
    (In Vitro)

    A number of other kinases are also similarly inhibited by AST 487 (NVP-AST487) in the in vitro kinase assays, including KDR (IC50=170 nM), Flt-4 (IC50=790 nM), Flt-3 (IC50=520 nM), c-Kit (IC50=500 nM), and c-Abl (IC50=20 nM). AST 487 potently inhibits the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations. Both GDNF/GFRα1 and persephin-induced calcitonin mRNA are markedly inhibited by coincubation with 100 nM of AST 487 in MTC-M cells[1]. AST 487 is a novel, mutant FLT3 inhibitor. AST 487 is tested in biochemical assays for inhibition of Flt-3 kinase activity. The Ki is determined to be 0.12 μM. Besides Flt-3, NVP-AST487 inhibits RET, KDR, c-Kit, and c-Abl kinase with IC50 values below 1 μM. Treatment of FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells with AST 487 potently inhibits cellular proliferation (IC50<5 nM). AST 487 treatment of FLT3-ITD-Ba/F3 cells with 0.01 μM AST 487 results in complete cell killing compare with approximately 50% killing of AML patient samples at the same concentration[2].

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

    AST 487 相关抗体:
    体内研究
    (In Vivo)

    After a single oral administration of 15 mg/kg of AST 487 to OF1 mice, a mean peak plasma level (Cmax) of 0.505±0.078 μM SE is achieved after 0.5 h. Similar levels of AST 487 are found in the plasma of mice up to 6 h after oral administration, with a Clast of 21±4 nM at 24 h. The oral bioavailability is calculated to be 9.7% with a t1/2 terminal elimination of 1.5 h[1].

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

    529.56

    Formula

    C26H30F3N7O2
    CAS 号
    性状

    固体

    颜色

    White to off-white

    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： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (188.84 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)

    * "≥" 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 1.8884 mL 9.4418 mL 18.8836 mL
    5 mM 0.3777 mL 1.8884 mL 3.7767 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.72 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。

      以 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。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.72 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。

      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。
    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
    参考文献
    Kinase Assay
    [1]

    Glutathione S-transferase (GST)-fused kinase domains are expressed in baculovirus and purified over glutathione-sepharose. Kinase activity is tested by measuring the phosphorylation of a synthetic substrate [poly(Glu, Tyr)], by purified GST-fusion kinase domains of the respective protein kinase in the presence of radiolabeled ATP; the ATP concentrations used are optimized within the Km range for the individual kinases. Briefly, each kinase is incubated under optimized buffer conditions in 20 mM of Tris-HCl (pH 7.5), 1 to 3 mM of MnCl2, 3 to 10 mM of MgCl2, 10 μM of Na3VO4, 1 mM of DTT, 0.2 μCi [33P]ATP, 1 to 8 μM of ATP, 3 to 8 μg/mL of poly(Glu/Tyr, 4:1), and 1% DMSO in a total volume of 30 μL in the presence or absence of NVP-AST487 for 10 min at ambient temperature. Reactions are terminated by adding 10 μL of 250 mM EDTA, and the reaction mixture is transferred onto an Immobilon polyvinylidene difluoride membrane. Filters are washed (0.5% H3PO4), soaked in ethanol, dried and counted in a liquid scintillation counter. IC50s for AST 487 are calculated by linear regression analysis of the percentage inhibition[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [2]

    The trypan blue exclusion assay is used to determine proliferation of cells cultured in the presence and absence of NVP-AST 487. Cell viability is reported as percentage of control (untreated) cells, and data are presented as the average of 2 independent experiments, except where indicated. Error bars represent the standard error of the mean for each data point. Apoptosis of drug-treated cells is measured using the Annexin-V-Fluos Staining Kit. Cell-cycle analysis is performed[2].

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

    Mice[1]
    Female athymic nude mice are kept under optimized hygienic conditions (maximum of 10 mice per Makrolon type III cage) with free access to food and water. Tumors are established by s.c. injection of 1×106 and 5×106 of NIH3T3-RETC634W and TT cells, respectively, in 100 μL of HBSS per mouse. Treatable tumors, i.e., mean tumor volume of 100 mm3, developed within 10 days of NIH3T3-RETC634W cell injection, and within 20 days of TT cell injection. NVP-AST487 is given p.o., once daily by gavage. The compound is formulated by dissolving the appropriate amount of powder in N-methylpyrrolidone/PEG300 (1:10 v/v). The mice are randomized into four treatment groups of eight mice each. The first three groups received daily oral administrations of NVP-AST487 at 50, 30, and 10 mg/kg, respectively, for 3 weeks. The fourth group received treatment with vehicle. Tumor growth and body weights are monitored twice weekly. Tumor volumes are determined according to the formula: length×diameter2×π/6. Tumors are collected and frozen in liquid nitrogen at the end of the efficacy study, 6 h after the last administration.

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

    AST 487 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 1 mM 1.8884 mL 9.4418 mL 18.8836 mL 47.2090 mL
    5 mM 0.3777 mL 1.8884 mL 3.7767 mL 9.4418 mL
    10 mM 0.1888 mL 0.9442 mL 1.8884 mL 4.7209 mL
    15 mM 0.1259 mL 0.6295 mL 1.2589 mL 3.1473 mL
    20 mM 0.0944 mL 0.4721 mL 0.9442 mL 2.3605 mL
    25 mM 0.0755 mL 0.3777 mL 0.7553 mL 1.8884 mL
    30 mM 0.0629 mL 0.3147 mL 0.6295 mL 1.5736 mL
    40 mM 0.0472 mL 0.2360 mL 0.4721 mL 1.1802 mL
    50 mM 0.0378 mL 0.1888 mL 0.3777 mL 0.9442 mL
    60 mM 0.0315 mL 0.1574 mL 0.3147 mL 0.7868 mL
    80 mM 0.0236 mL 0.1180 mL 0.2360 mL 0.5901 mL
    100 mM 0.0189 mL 0.0944 mL 0.1888 mL 0.4721 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:

    AST 487630124-46-8NVP-AST 487AST487AST-487RETFLT3VEGFRc-KitBcr-AblCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Vascular endothelial growth factor receptorSCFRCD117Inhibitorinhibitorinhibit

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