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

TAK-632 是一種有效的 pan-RAF 抑制劑，作用于 CRAF，BRAFV600E 和 BRAFWT，IC50 分別為 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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     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥793
In-stock
1 mg ￥300
In-stock
5 mg ￥650
In-stock
10 mg ￥990
In-stock
25 mg ￥1950
In-stock
50 mg ￥2950
In-stock
100 mg ￥3988
In-stock
200 mg ￥5838
In-stock
500 mg   詢價  
1 g   詢價  

* Please select Quantity before adding items.

Customer Review

    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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    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-375 IC50
    12 nM
    Compound: 8B, TAK-632
    Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of MEK after 2 hrs by Western blotting analysis
    Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of MEK after 2 hrs by Western blotting analysis
    		[PMID: 23906342]
    A-375 IC50
    16 nM
    Compound: 8B, TAK-632
    Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of ERK after 2 hrs by Western blotting analysis
    Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of ERK after 2 hrs by Western blotting analysis
    		[PMID: 23906342]
    A-375 IC50
    160 nM
    Compound: 127; TAK-632
    Antiproliferative activity against human A-375 cells harbouring B-Raf V600E mutant by SRB assay
    Antiproliferative activity against human A-375 cells harbouring B-Raf V600E mutant by SRB assay
    		[PMID: 32798788]
    A-375 GI50
    66 nM
    Compound: 8B, TAK-632
    Antiproliferative activity against human A375 cells assessed as growth inhibition after 72 hrs by chemi-luminescence cell viability assay
    Antiproliferative activity against human A375 cells assessed as growth inhibition after 72 hrs by chemi-luminescence cell viability assay
    		[PMID: 23906342]
    A549 IC50
    8.5 μM
    Compound: TAK-632
    Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTS assay
    Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTS assay
    		[PMID: 26745854]
    CHL-1 IC50
    2.07 nM
    Compound: 127; TAK-632
    Antiproliferative activity against human CHL-1 cells harbouring wild type B-Raf by SRB assay
    Antiproliferative activity against human CHL-1 cells harbouring wild type B-Raf by SRB assay
    		[PMID: 32798788]
    COLO 205 IC50
    0.025 μM
    Compound: 3; TAK-632
    Cytotoxicity against human COLO205 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human COLO205 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 27155899]
    HCT-116 IC50
    0.362 μM
    Compound: 3; TAK-632
    Cytotoxicity against human HCT116 cells harboring wild type B-Raf assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells harboring wild type B-Raf assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 27155899]
    HMCB cell line IC50
    350 nM
    Compound: 127; TAK-632
    Antiproliferative activity against human HMCB cells harbouring wild type B-Raf by SRB assay
    Antiproliferative activity against human HMCB cells harbouring wild type B-Raf by SRB assay
    		[PMID: 32798788]
    HMV-2 cell line IC50
    200 nM
    Compound: 127; TAK-632
    Antiproliferative activity against human HMV-2 cells harbouring B-Raf G469V mutant by SRB assay
    Antiproliferative activity against human HMV-2 cells harbouring B-Raf G469V mutant by SRB assay
    		[PMID: 32798788]
    HMV-2 cell line GI50
    200 nM
    Compound: 8B, TAK-632
    Antiproliferative activity against human HMVII cells assessed as growth inhibition after 72 hrs by chemi-luminescence cell viability assay
    Antiproliferative activity against human HMVII cells assessed as growth inhibition after 72 hrs by chemi-luminescence cell viability assay
    		[PMID: 23906342]
    HT-144 IC50
    110 nM
    Compound: 127; TAK-632
    Antiproliferative activity against human HT-144 cells harbouring B-Raf V600E mutant by SRB assay
    Antiproliferative activity against human HT-144 cells harbouring B-Raf V600E mutant by SRB assay
    		[PMID: 32798788]
    HT-29 CC50
    > 50 μM
    Compound: 6; TAK-632
    Cytotoxicity against human HT-29 cells measured after 12 hrs by CellTiter-Glo Luminescent assay
    Cytotoxicity against human HT-29 cells measured after 12 hrs by CellTiter-Glo Luminescent assay
    		[PMID: 31095385]
    HT-29 IC50
    0.033 μM
    Compound: 3; TAK-632
    Cytotoxicity against human HT-29 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HT-29 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 27155899]
    HT-29 EC50
    1.44 μM
    Compound: 6; TAK-632
    Anti-necroptotic activity in human HT-29 cells assessed as inhibition of NFalpha/SM-164/Z-VAD-fmk-induced necroptosis measured after 12 hrs by celltiter-glo luminescent cell viability assay
    Anti-necroptotic activity in human HT-29 cells assessed as inhibition of NFalpha/SM-164/Z-VAD-fmk-induced necroptosis measured after 12 hrs by celltiter-glo luminescent cell viability assay
    		[PMID: 31095385]
    HT-29 EC50
    1.44 μM
    Compound: TAK-632; 75
    Anti-necrotic activity in TSZ induced human HT-29 cells incubated for 16 hrs in presence of TSZ by flow cytometry analysis
    Anti-necrotic activity in TSZ induced human HT-29 cells incubated for 16 hrs in presence of TSZ by flow cytometry analysis
    		[PMID: 36346971]
    HT-29 EC50
    1440 nM
    Compound: TAK-632
    Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TCZ)-induced necroptosis pretreated for 8 to 12 hrs
    Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TCZ)-induced necroptosis pretreated for 8 to 12 hrs
    		[PMID: 33964444]
    Malme-3M IC50
    50 nM
    Compound: 127; TAK-632
    Antiproliferative activity against human Malme-3M cells harbouring B-Raf V600E mutant by SRB assay
    Antiproliferative activity against human Malme-3M cells harbouring B-Raf V600E mutant by SRB assay
    		[PMID: 32798788]
    SK-MEL-2 IC50
    60 nM
    Compound: 127; TAK-632
    Antiproliferative activity against human SK-MEL-2 cells harbouring wild type B-Raf by SRB assay
    Antiproliferative activity against human SK-MEL-2 cells harbouring wild type B-Raf by SRB assay
    		[PMID: 32798788]
    體外研究
    (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.
    體內(nèi)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 號
    性狀

    固體

    顏色

    White to off-white

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實驗： 

    DMSO 中的溶解度 : 100 mg/mL (180.34 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (4.51 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.51 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料
    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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
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    • 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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    Inquiry Information

    產(chǎn)品名稱：
    TAK-632
    目錄號：
    HY-15767
    需求量：