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  2. MAPK/ERK Pathway Autophagy
  3. Raf Autophagy
  4. LY3009120

LY3009120 (DP-4978) 是泛 RAF 抑制劑，其抑制BRAFV600E，BRAFWT 和CRAFWT 的 IC50 分別為 5.8，9.1和15 nM。

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LY3009120 Chemical Structure

LY3009120 Chemical Structure

CAS No. : 1454682-72-4

1.  客戶無需承擔(dān)相應(yīng)的運輸費用。

2.  同一機(jī)構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機(jī)構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥794
In-stock
1 mg ￥386
In-stock
5 mg ￥850
In-stock
10 mg ￥1350
In-stock
25 mg ￥2700
In-stock
50 mg ￥4000
In-stock
100 mg ￥5438
In-stock
200 mg 現(xiàn)貨 詢價
500 mg   詢價  
1 g   詢價  

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Customer Review

    LY3009120 purchased from MCE. Usage Cited in: Clin Sci (Lond). 2019 Apr 16;133(8):919-932.  [Abstract]

    Colonic proteins on day 7 are tested by immunoblotting to detect p-MLKL, MLKL and cleaved caspase-3 with corresponding antibodies. GAPDH is used as an internal control. Three individual mice from each group are shown.

    LY3009120 purchased from MCE. Usage Cited in: Clin Sci (Lond). 2019 Apr 16;133(8):919-932.  [Abstract]

    LY3009120 decreases phosphorylation of RIPK1, RIPK3 and MLKL in T/S/Z treated HT-29 cells. HT-29 cells are pretreated with DMSO or LY3009120 for 1 hour, then treated with T/S/Z for 0, 2, 4 and 6 hours, respectively.

    LY3009120 purchased from MCE. Usage Cited in: Oncogene. 2018 Oct;37(43):5719-5734.  [Abstract]

    BRAF mutants with in-frame β3-αC loop deletions have approximate sensitivities to RAF dimer inhibitor, LY3009120.

    查看 Raf 亞型特異性產(chǎn)品:

    • 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

    LY3009120 (DP-4978) is a pan RAF inhibitor which inhibits BRAFV600E, BRAFWT and CRAFWT with IC50s of 5.8, 9.1 and 15 nM, respectively.

    IC50 & Target[1]

    BRafV600E

    5.8 nM (IC50)

    Braf

    9.1 nM (IC50)

    CRAF

    15 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-375 IC50
    0.0092 μM
    Compound: 13, LY3009120
    Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay
    Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay
    		[PMID: 25965804]
    A-375 IC50
    0.037 μM
    Compound: 13, LY3009120
    Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay
    Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay
    		[PMID: 25965804]
    A-375 IC50
    0.3 μM
    Compound: LY3009120
    Antiproliferative activity against human A375 cells after 72 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human A375 cells after 72 hrs by Cell-Titer Glo assay
    		[PMID: 30529543]
    A-375 IC50
    100 nM
    Compound: 13, LY3009120
    Competitive binding affinity to EphB4 in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to EphB4 in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    20 nM
    Compound: 13, LY3009120
    Competitive binding affinity to EphA2 in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to EphA2 in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    28.3 nM
    Compound: 1; LY3009120
    Antiproliferative activity against human A-375 cells harboring BRAF mutant assessed as reduction in cell viability incubated for 24 hrs by Click-iT EdU cell proliferation imaging assay
    Antiproliferative activity against human A-375 cells harboring BRAF mutant assessed as reduction in cell viability incubated for 24 hrs by Click-iT EdU cell proliferation imaging assay
    		[PMID: 33780623]
    A-375 IC50
    290 nM
    Compound: 13, LY3009120
    Competitive binding affinity to CSK in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to CSK in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    31 nM
    Compound: 13, LY3009120
    Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    310 nM
    Compound: 13, LY3009120
    Competitive binding affinity to SRC in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to SRC in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    380 nM
    Compound: 13, LY3009120
    Competitive binding affinity to ABL in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to ABL in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    39 nM
    Compound: 13, LY3009120
    Competitive binding affinity to ZAK in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to ZAK in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    390 nM
    Compound: 13, LY3009120
    Competitive binding affinity to IRAK1 in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to IRAK1 in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 EC50
    4.36 mg/kg
    Compound: 13, LY3009120
    In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed NIH nude rat assessed as inhibition of ERK phosphorylation by ELISA
    In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed NIH nude rat assessed as inhibition of ERK phosphorylation by ELISA
    		[PMID: 25965804]
    A-375 IC50
    42 nM
    Compound: 13, LY3009120
    Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    44 nM
    Compound: 13, LY3009120
    Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    450 nM
    Compound: 13, LY3009120
    Competitive binding affinity to GCN2 in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to GCN2 in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    470 nM
    Compound: 13, LY3009120
    Competitive binding affinity to JNK in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to JNK in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    61 nM
    Compound: 13, LY3009120
    Competitive binding affinity to p38 in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to p38 in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    800 nM
    Compound: 13, LY3009120
    Competitive binding affinity to MAP2K5 in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to MAP2K5 in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    91 nM
    Compound: 13, LY3009120
    Competitive binding affinity to FYN in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to FYN in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    970 nM
    Compound: 13, LY3009120
    Competitive binding affinity to KHS1 in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to KHS1 in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    98 nM
    Compound: 13, LY3009120
    Competitive binding affinity to MAP3K1 in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to MAP3K1 in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A549 IC50
    45.6 nM
    Compound: 1; LY3009120
    Synergistic antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability incubated for 24 hrs in presence of 100 nM cobimetinib by Click-iT EdU cell proliferation imaging assay
    Synergistic antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability incubated for 24 hrs in presence of 100 nM cobimetinib by Click-iT EdU cell proliferation imaging assay
    		[PMID: 33780623]
    A549 IC50
    545 nM
    Compound: 1; LY3009120
    Antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability incubated for 24 hrs by Click-iT EdU cell proliferation imaging assay
    Antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability incubated for 24 hrs by Click-iT EdU cell proliferation imaging assay
    		[PMID: 33780623]
    HCT-116 IC50
    0.15 μM
    Compound: 13, LY3009120
    Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA
    Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA
    		[PMID: 25965804]
    HCT-116 IC50
    0.22 μM
    Compound: 13, LY3009120
    Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay
    Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay
    		[PMID: 25965804]
    HepG2 IC50
    2.6 μM
    Compound: LY3009120
    Antiproliferative activity against human HepG2 cells after 72 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human HepG2 cells after 72 hrs by Cell-Titer Glo assay
    		[PMID: 30529543]
    HT-29 IC50
    0.9 μM
    Compound: LY3009120
    Antiproliferative activity against human HT-29 cells after 72 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human HT-29 cells after 72 hrs by Cell-Titer Glo assay
    		[PMID: 30529543]
    MV4-11 IC50
    0.1 μM
    Compound: LY3009120
    Antiproliferative activity against human MV4-11 cells after 72 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human MV4-11 cells after 72 hrs by Cell-Titer Glo assay
    		[PMID: 30529543]
    SK-MEL-2 IC50
    0.2 μM
    Compound: LY3009120
    Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by Cell-Titer Glo assay
    		[PMID: 30529543]
    體外研究
    (In Vitro)

    In the whole-cell based KiNativ assay, LY3009120 shows affinity to each RAF isoform with the IC50 of 44, 31-47 and 42 nM for ARAF, BRAF and CRAF respectively. LY3009120 exhibits anti-proliferative effects on cell lines harboring BRAFV600E, KRASG13 and KRASG12 mutations. LY3009120 (1 μM) inhibits the phosphorylation of both MEK1/2 and ERK1/2 in cell lines with high basal levels of pMEK1/2 and pERK1/2 (RKO and HCT 116)[1]. LY3009120 shows inhibitory effect on tumor cells such as BxPC-3, NCI-H2405 and OV-90 cell lines. LY3009120 (0.01 μM) demonstrates potent and dose-dependent inhibition of phospho-MEK and ERK in all three cell lines. LY3009120 demonstrates a concentration-dependent cell growth inhibition with IC50 values of 0.04, 0.087, and 0.007 μM against H2405, BxPC-3, and OV-90 cells, respectively[2]. LY3009120 inhibits BRAFWT, CRAFWT, BRAFV600E, and BRAFV600E+G468A with the IC50 values of 9.1, 15, 5.8, and 17 nM, respectively. LY3009120 induces BRAF-CRAF dimerization but inhibits the phosphorylation of downstream MEK and ERK. LY3009120 also inhibits various forms of RAF dimers including BRAF or CRAF homodimers[3]. LY3009120 gives only very minor activation at very low doses, with near complete inhibition of phospho-ERK at concentrations above 100 nM[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    LY3009120 (20 mg/kg bid) displays significant activity in in vivo BRAFmut and KRASmut CRC xenograft models. In Colo 205 xenografts (BRAFmut), LY3009120 results in statistically significant tumor regression, while treatment of HCT 116 xenografts (KRASmut) results in statistically significant inhibition of tumor growth. LY3009120 treatment reduces pMEK1/2 in all HT-29 xenografts and reduces pERK1/2 in the majority of HT-29 xenografts[1]. LY3009120 (15 or 30 mg/kg) achieves almost complete tumor growth regression, and inhibits downstream phospho-MEK and ERK by approximately 70% and 60%, respectively, in the H2405 model[2].

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

    424.51

    Formula

    C23H29FN6O
    CAS 號
    性狀

    固體

    顏色

    Light yellow to khaki

    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 : ≥ 38 mg/mL (89.51 mM; 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)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.3557 mL 11.7783 mL 23.5566 mL
    5 mM 0.4711 mL 2.3557 mL 4.7113 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： 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.89 mM); 懸濁液; 超聲助溶

    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

    純度: 98.66%

    參考文獻(xiàn)
    Cell Assay
    [4]

    Briefly, cells are grown in McCoy’s 5A supplemented with 10% characterized fetal bovine serum at 37°C, 5% CO2, and 95% humidity. Cells are allowed to expand until 75-90% confluency at which point they are subcultured or harvested for assay use. A serial dilution of test compound is dispensed into a 384-well black clear bottom plate in triplicate. Six-hundred-twenty-five cells are added per well in 50 μL of complete growth medium in the 384-well plate. Plates are incubated for 67 h at 37°C, 5% CO2, and 95% humidity. At the end of the incubation period, 10 μL of a 440 μM solution of resazurin in PBS is added to each well of the plate and plates are incubated for an additional 5 h at 37°C, 5% CO2, and 95% humidity. Plates are read on a Synergy2 reader using an excitation of 540 nm and an emission of 600 nm. Data are analyzed using Prism softwareto calculate IC50 values.

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

    Briefly, 5×106 to 10×106 tumor cells in a 1:1 Matrigel mix (0.2 mL total volume) are injected subcutaneously into the right hind flank of female NIH nude rats. After tumors reach a desired size of approximately 300 mm3, animals are randomized into groups of 8 for efficacy studies. Drugs (LY3009120 or PLX4032) are administered orally (gavage) in 0.6-mL volume of vehicle with the dose schedules. Tumor growth and body weight are monitored over time to evaluate efficacy and signs of toxicity.

    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 2.3557 mL 11.7783 mL 23.5566 mL 58.8914 mL
    5 mM 0.4711 mL 2.3557 mL 4.7113 mL 11.7783 mL
    10 mM 0.2356 mL 1.1778 mL 2.3557 mL 5.8891 mL
    15 mM 0.1570 mL 0.7852 mL 1.5704 mL 3.9261 mL
    20 mM 0.1178 mL 0.5889 mL 1.1778 mL 2.9446 mL
    25 mM 0.0942 mL 0.4711 mL 0.9423 mL 2.3557 mL
    30 mM 0.0785 mL 0.3926 mL 0.7852 mL 1.9630 mL
    40 mM 0.0589 mL 0.2945 mL 0.5889 mL 1.4723 mL
    50 mM 0.0471 mL 0.2356 mL 0.4711 mL 1.1778 mL
    60 mM 0.0393 mL 0.1963 mL 0.3926 mL 0.9815 mL
    80 mM 0.0294 mL 0.1472 mL 0.2945 mL 0.7361 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.

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    Inquiry Information

    產(chǎn)品名稱：
    LY3009120
    目錄號：
    HY-12558
    需求量：