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  2. PI3K/Akt/mTOR
  3. PI3K
  4. Alpelisib

Alpelisib (BYL-719) 是有效，選擇性的，具有口服活性的 PI3Kα 抑制劑。Alpelisib (BYL-719) 對(duì) PIK3CA 突變癌具有靶向性。Alpelisib (BYL-719) 抑制 p110α、p110γ、p110δ、p110β 的 IC50 分別為 5 nM，250 nM，290 nM，1200 nM。具有抗腫瘤活性。

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Alpelisib Chemical Structure

Alpelisib Chemical Structure

CAS No. : 1217486-61-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥825
In-stock
5 mg ￥750
In-stock
10 mg ￥1280
In-stock
50 mg ￥3600
In-stock
100 mg ￥5500
In-stock
200 mg 現(xiàn)貨 詢價(jià)
500 mg   詢價(jià)  
1 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Alpelisib:

MCE 顧客使用本產(chǎn)品發(fā)表的 94 篇科研文獻(xiàn)

WB

    Alpelisib purchased from MCE. Usage Cited in: Cancer Lett. 2019 Jan;440-441:54-63.  [Abstract]

    The siNC- or siBTF3-transfected breast cancer cells are treated with BYL-719 and are then subjected to an immunoblotting analysis.

    Alpelisib purchased from MCE. Usage Cited in: Nature. 2018 Jun;558(7711):540-546.  [Abstract]

    Western blot of P-AKT (Ser473), P-AKT (Thr308) and P-S6RP in liver, heart and muscles, respectively, from PIK3CAWT and PIK3CACAGG-CreER mice treated with or without BYL719 directly after Cre induction (preventive) or seven days later (therapeutic).

    Alpelisib purchased from MCE. Usage Cited in: Oncogene. 2016 Jul 7;35(27):3607-12.  [Abstract]

    (A) Immunoblot analyses in HCC1569 cells treated with BYL719, KIN193 (MedChemexpress) or BKM120 (μM). (B, C) Immunoblot analyses in BT474 and BT474-shPTEN cells treated as indicated in (A).

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity[1][2][3].

    IC50 & Target[1][2]

    p110α

    5 nM (IC50)

    p110γ

    250 nM (IC50)

    p110δ

    290 nM (IC50)

    p110β

    1200 nM (IC50)

    p110α-H1047R

    4 nM (IC50)

    p110α-E545K

    4 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Kasumi 1 IC50
    0.44 μM
    Compound: Alpelisib
    Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
    Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
    		[PMID: 37126967]
    MCF7 IC50
    0.43 μM
    Compound: Alpelisib
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 35834807]
    MCF7 IC50
    530 nM
    Compound: 2; BYL719
    Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay
    Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay
    		[PMID: 33356246]
    MDA-MB-231 IC50
    62.9 μM
    Compound: Alpesilib
    Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs
    Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs
    		[PMID: 33139111]
    MGC-803 IC50
    0.43 μM
    Compound: Alpelisib
    Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
    		[PMID: 35834807]
    Rat1 IC50
    0.074 μM
    Compound: 8, NVP-BYL719
    Inhibition of N-terminal myristoylated P110alpha (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA
    Inhibition of N-terminal myristoylated P110alpha (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA
    		[PMID: 23726034]
    Rat1 IC50
    0.074 μM
    Compound: 1, BYL719
    Inhibition of myristoylated human P110alpha expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis
    Inhibition of myristoylated human P110alpha expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis
    		[PMID: 26164189]
    Rat1 IC50
    1.2 μM
    Compound: 8, NVP-BYL719
    Inhibition of N-terminal myristoylated P110delta (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA
    Inhibition of N-terminal myristoylated P110delta (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA
    		[PMID: 23726034]
    Rat1 IC50
    1.2 μM
    Compound: 1, BYL719
    Inhibition of myristoylated human P110delta expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis
    Inhibition of myristoylated human P110delta expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis
    		[PMID: 26164189]
    Rat1 IC50
    2.2 μM
    Compound: 8, NVP-BYL719
    Inhibition of N-terminal myristoylated P110beta (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA
    Inhibition of N-terminal myristoylated P110beta (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA
    		[PMID: 23726034]
    Rat1 IC50
    2.2 μM
    Compound: 1, BYL719
    Inhibition of myristoylated human P110beta expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis
    Inhibition of myristoylated human P110beta expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis
    		[PMID: 26164189]
    SJRH30 IC50
    7.6 μM
    Compound: BYL719
    Antiproliferative activity against human Rh30 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human Rh30 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    		[PMID: 33109399]
    T47D IC50
    0.1 μM
    Compound: Alpelisib
    Antiproliferative activity against human T47D cells expressing PIK3CA mutant assessed as cell growth inhibition incubated for 72 hrs by MTT assay
    Antiproliferative activity against human T47D cells expressing PIK3CA mutant assessed as cell growth inhibition incubated for 72 hrs by MTT assay
    		[PMID: 37126967]
    T47D IC50
    420 nM
    Compound: 2; BYL719
    Antiproliferation activity against human T47D cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay
    Antiproliferation activity against human T47D cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay
    		[PMID: 33356246]
    體外研究
    (In Vitro)

    Alpelisib (BYL-719) 有效抑制 2 種最常見(jiàn)的 PIK3CA 體細(xì)胞突變 (H1047R、E545K；IC50~4 nM)。Alpelisib 有效抑制 PI3Kα 轉(zhuǎn)化細(xì)胞中的 Akt 磷酸化 (IC50=74±15 nM)，并且在 PI3Kβ 或 PI3Kδ 亞型轉(zhuǎn)化細(xì)胞中顯示出顯著降低的抑制活性 (與 PI3Kα 相比≥15 倍)[2]。
    Alpelisib (BYL-719，0-50 μM；72 小時(shí)) 以劑量依賴性方式抑制骨肉瘤細(xì)胞系 MG63、HOS、POS-1 和 MOS-J 的細(xì)胞生長(zhǎng)[3]。
    Alpelisib (BYL-719) 顯著改變細(xì)胞周期階段的分布。Alpelisib (BYL-719，25 μM；18 小時(shí)) 誘導(dǎo)人和小鼠骨肉瘤細(xì)胞系的 G0/G1 期細(xì)胞周期停滯[3]。

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

    Cell Proliferation Assay[3]

    Cell Line: MG63, HOS, POS-1, MOS-J
    Concentration: 10, 20, 30, 40, 50 μM
    Incubation Time: 72 hours
    Result: Inhibited the cell growth of all osteosarcoma cell lines tested in a dose-dependent manner with IC50s of 6-15 μM and with IC90s of 24-42 μM.

    Cell Cycle Analysis[3]

    Cell Line: MG63, HOS, POS-1, MOS-J
    Concentration: 25 μM
    Incubation Time: 18 hours
    Result: Induced a cell cycle arrest in the G0/G1 phase of human and murine osteosarcoma cell .
    體內(nèi)研究
    (In Vivo)

    Alpelisib 對(duì)大鼠 (1 mg/kg，iv) 具有中等的終末消除半衰期 (t1/2=2.9±0.2 h)[1]。
    Alpelisib (BYL-719) (C57Bl/6J 小鼠為 12.5 mg/kg 和 50 mg/kg；雌性 Rj:NMRI 裸鼠為 50 mg/kg；口服給藥；每天) 顯著減少腫瘤體積和異位骨基質(zhì)的沉積[3]。

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

    Animal Model: A 5-week-old female Rj:NMRI-nude mice with human HOS-MNNG osteosarcoma cells; A 5-week-old male C57Bl/6J mice with mouse MOS-J osteosarcoma cells[3]
    Dosage: 12.5 mg/kg and 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude mice
    Administration: Oral administration; daily; 22 or 29 days for C57Bl/6J mice or Rj:NMRI-nude mice
    Result: Significantly reduced tumor volumes and simultaneously reduced tumor growth.
    Animal Model: Female Sprague Dawley rats [1]
    Dosage: 1 mg/kg (Pharmacokinetic Analysis)
    Administration: I.V.
    Result: t1/2=2.9±0.2 hours.
    Clinical Trial
    分子量

    441.47

    Formula

    C19H22F3N5O2S
    CAS 號(hào)
    性狀

    固體

    顏色

    Off-white to light yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)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(shí)驗(yàn)： 

    DMSO 中的溶解度 : 83.33 mg/mL (188.76 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.2652 mL 11.3258 mL 22.6516 mL
    5 mM 0.4530 mL 2.2652 mL 4.5303 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)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(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)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(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 5 mg/mL (11.33 mM); 澄清溶液

    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (4.71 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 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 20.8 mg/mL 的澄清 DMSO 儲(chǔ)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。

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 0.5% Methyl cellulose/0.5% Tween-80 in Saline water

      Solubility: 10 mg/mL (22.65 mM); Suspension solution; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑： 1% CMC/0.5% Tween-80 in Saline water

      Solubility: 10 mg/mL (22.65 mM); Suspension solution; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)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(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)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(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)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: 99.95%

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?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 2.2652 mL 11.3258 mL 22.6516 mL 56.6290 mL
    5 mM 0.4530 mL 2.2652 mL 4.5303 mL 11.3258 mL
    10 mM 0.2265 mL 1.1326 mL 2.2652 mL 5.6629 mL
    15 mM 0.1510 mL 0.7551 mL 1.5101 mL 3.7753 mL
    20 mM 0.1133 mL 0.5663 mL 1.1326 mL 2.8314 mL
    25 mM 0.0906 mL 0.4530 mL 0.9061 mL 2.2652 mL
    30 mM 0.0755 mL 0.3775 mL 0.7551 mL 1.8876 mL
    40 mM 0.0566 mL 0.2831 mL 0.5663 mL 1.4157 mL
    50 mM 0.0453 mL 0.2265 mL 0.4530 mL 1.1326 mL
    60 mM 0.0378 mL 0.1888 mL 0.3775 mL 0.9438 mL
    80 mM 0.0283 mL 0.1416 mL 0.2831 mL 0.7079 mL
    100 mM 0.0227 mL 0.1133 mL 0.2265 mL 0.5663 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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    產(chǎn)品名稱：
    Alpelisib
    目錄號(hào)：
    HY-15244
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