2. MAPK/ERK Pathway Epigenetics Cell Cycle/DNA Damage
  3. Raf Aurora Kinase
  4. TAK-632

TAK-632 是一种有效的 pan-RAF 抑制剂，作用于 CRAF，BRAFV600E 和 BRAFWT，IC50 分别为 1.4，2.4 和 8.3 nM。

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TAK-632 Chemical Structure

TAK-632 Chemical Structure

CAS No. : 1228591-30-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1090
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1 mg ￥300
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5 mg ￥650
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10 mg ￥990
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25 mg ￥1950
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50 mg ￥2950
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100 mg ￥3988
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500 mg   询价  

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Customer Review

TAK-632 相关抗体

Top Publications Citing Use of Products

    TAK-632 purchased from MCE. Usage Cited in: Br J Pharmacol. 2019 Jun;176(12):2095-2108.  [Abstract]

    L929 cells are pretreated with TAK-632 (5 μM) followed by stimulated with mTNF-α (20 ng) plus z-VAD-FMK (20 μM) (TZ) at the indicated time points. Cells are lysed and immunoblotted with the indicated antibodies.

    TAK-632 purchased from MCE. Usage Cited in: Br J Pharmacol. 2019 Jun;176(12):2095-2108.  [Abstract]

    HT-29 cells are pretreated with TAK-632 (10 μM) followed by stimulation with TSZ at the indicated time points. Cells are lysed and immunoblotted with the indicated antibodies.

    TAK-632 purchased from MCE. Usage Cited in: Br J Pharmacol. 2019 Jun;176(12):2095-2108.  [Abstract]

    HEK293T cells are transfected with FLAG-RIPK1 or RIPK3-V5. After 12 h, the cells are treated with TAK-632 as the indicated concentrations for 6 h. Cell lysates are then analyzed by SDS-PAGE and immunoblotted with the indicated antibodies. All western data are representative of five independent experiments.

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    Aurora Kinase Aurora A Aurora B Aurora C

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAFV600E, BRAFWT, respectively.

    IC50 & Target[1]

    c-Raf

    1.4 nM (IC50)

    Braf

    8.3 nM (IC50)

    Aurora B

    66 nM (IC50)

    PDGFRβ

    120 nM (IC50)

    PDGFRα

    610 nM (IC50)

    FGFR3

    280 nM (IC50)

    TIE2

    740 nM (IC50)

    IKKβ

    3700 nM (IC50)

    CDK1

    790 nM (IC50)

    CDK2

    580 nM (IC50)

    p38α

    600 nM (IC50)

    GSK3β

    500 nM (IC50)

    MEK1

    3700 nM (IC50)

    体外研究
    (In Vitro)

    TAK-632 inhibits PDGFRβ, FGFR3, GSK3β, CDK2, P38α, PDGFRα, TIE2, and CDK1 with a range of IC50 values from 120-790 nM. CHK1, IKKβ, and MEK1 are inhibited over an IC50 range of 1400-1700 nM. With 1 h of preincubation time, TAK-632 inhibits BRAF and CRAF in an ATP competitive manner (at low ATP concentrations BRAF IC50: 15 nM; CRAF: 8.1 nM). The respective biochemical activity of TAK-632 against BRAF and CRAF reduces to IC50 values of 58 nM and 62 nM at high ATP concentrations.TAK-632 demonstrates strong inhibition of pMEK and pERK in HMVII cells with IC50 values of 49 nM and 50 nM, respectively[1]. TAK-632 shows strong antiproliferative effects both in A375 and SK-MEL-2 cells (GI50 of 40-190 nM in A375 cells and GI50 of 190-250 nM in SK-MEL-2 cells)[2].

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

    TAK-632 相关抗体:
    体内研究
    (In Vivo)

    TAK-632 demonstrates dramatically improved solubility (740 μg/mL) in pH 6.8 phosphate buffer and exhibits significant oral absorption (at a dose of 25 mg/kg, AUC, 32.47 μg h/mL; F, 51.7%) in rats. In a dog PK study, 10 mg/kg administration of TAK-632 also shows superior oral bioavailability (F: 108%).Oral single administration of TAK-632 inhibits pERK in tumors at 8 h after its administration over a dose range of 1.9-24.1 mg/kg. In particular, 9.7-24.1 mg/kg dosing with TAK-632 strongly inhibits pERK levels to 11% of the control. TAK-632 exhibits dose-dependent antitumor efficacy without severe body weight reduction over a dose range of 3.9-24.1 mg/kg. Significant tumor regression is observed at 9.7 mg/kg and 24.1 mg/kg (T/C=−2.1% and −12.1%, respectively)[1]. TAK-632 exhibits potent antitumor efficacy when orally administered at 60 mg/kg once daily (T/C=37%, P<0.001) or at 120 mg/kg once daily (T/C=29%, P<0.001) for 21 days without severe toxicity in NRAS-mutant melanoma using a SK-MEL-2 xenograft model[2].

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

    554.52

    Formula

    C27H18F4N4O3S
    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 (180.34 mM; 超声助溶; 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 1.8034 mL 9.0168 mL 18.0336 mL
    5 mM 0.3607 mL 1.8034 mL 3.6067 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 (4.51 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 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 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.51 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，此方案实验周期在半个月以上的动物实验酌情使用。

      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

    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
    [2]

    Immunoprecipitated BRAF or CRAF is incubated with recombinant inactive MEK (K97R) at 30°C for 30 minutes in kinase reaction buffer containing ATP/Mg2+. RAS/RAF wild-type (A431, CsFb, and HeLa), KRAS-mutant (A549, HCT-116, and MIA PaCa-2), and NRAS-mutant melanoma (GAK, HMV-II, and SK-MEL-2) cells are treated with TAK-632 (0, 0.32, 1.6, 8, 40, 200, 1000 and 5000 nM) at the indicated concentrations for 2 hours. Cell lysates are analyzed by Western blot analysis[2].

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

    Cell viability is assessed (3 replicates) using the Sulforhodamine B assay or by the CellTiter-Glo luminescent cell viability assay. The concentrations of TAK-632 that produced 50% growth inhibition (GI50) are calculated using PCP software. The combination index (CI) is calculated using CalcuSyn software. To investigate the antiproliferative activity of TAK-632, we performed proliferation assays in various cell lines harboring mutated BRAF, NRAS, or KRAS. HMV-II, SK-MEL-2, or A375 cells are cotreated with TAK-632 and TAK-733 at the indicated concentrations for 72 hours. Cell viability is measured. The CI value at EC50 is calculated. A375 cells stably expressing NRASQ61K or ΔN-BRAF are cotreated with TAK-632 and TAK-733 at the indicated concentrations for 72 hours. Cell viability is measured. The CI value at EC50 is calculated[2].

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

    Mice[2]
    The xenograft-implanted nude mice are used. Mice bearing SK-MEL-2 xenografts are treated once daily for 21 consecutive days with vehicle or TAK-632 at the indicated concentrations (10 mice per each treatment group). Day 0 indicates the beginning of treatment. Tumors are measured twice a week. Mice bearing SK-MEL-2 xenografts are treated once daily (QD) for 3 days with vehicle, TAK-632 at 60 mg/kg (60 mpk), or TAK-632 at 120 mg/kg (120 mpk). Tumor xenografts are obtained at indicated time points after the final treatment and analyzed by Western blot analysis. Individual blots with dividing lines are combined from a single electrophoresis gel. Bars represent densitometric analysis of phospho-ERK, normalized to vehicle-treated control (mean±SD).

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

    TAK-632 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 1.8034 mL 9.0168 mL 18.0336 mL 45.0840 mL
    5 mM 0.3607 mL 1.8034 mL 3.6067 mL 9.0168 mL
    10 mM 0.1803 mL 0.9017 mL 1.8034 mL 4.5084 mL
    15 mM 0.1202 mL 0.6011 mL 1.2022 mL 3.0056 mL
    20 mM 0.0902 mL 0.4508 mL 0.9017 mL 2.2542 mL
    25 mM 0.0721 mL 0.3607 mL 0.7213 mL 1.8034 mL
    30 mM 0.0601 mL 0.3006 mL 0.6011 mL 1.5028 mL
    40 mM 0.0451 mL 0.2254 mL 0.4508 mL 1.1271 mL
    50 mM 0.0361 mL 0.1803 mL 0.3607 mL 0.9017 mL
    60 mM 0.0301 mL 0.1503 mL 0.3006 mL 0.7514 mL
    80 mM 0.0225 mL 0.1127 mL 0.2254 mL 0.5636 mL
    100 mM 0.0180 mL 0.0902 mL 0.1803 mL 0.4508 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:

    TAK-6321228591-30-7TAK632TAK 632RafAurora KinaseRaf kinasesInhibitorinhibitorinhibit

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    目录号：
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