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  2. Cell Cycle/DNA Damage
  3. CDK
  4. Abemaciclib methanesulfonate

Abemaciclib methanesulfonate  (Synonyms: LY2835219 methanesulfonate)

目錄號(hào): HY-16297 純度: 99.90%
COA 產(chǎn)品使用指南

Abemaciclib methanesulfonate (LY2835219 methanesulfonate) 是選擇性的 CDK4/6 抑制劑，抑制 CDK4/CDK6 的 IC50 分別為 2 nM 和 10 nM。

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Abemaciclib methanesulfonate Chemical Structure

Abemaciclib methanesulfonate Chemical Structure

CAS No. : 1231930-82-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥800
In-stock
5 mg ￥600
In-stock
10 mg ￥900
In-stock
50 mg ￥1200
In-stock
100 mg ￥1500
In-stock
200 mg ￥1900
In-stock
500 mg ￥3500
In-stock
1 g   詢價(jià)  
5 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Abemaciclib methanesulfonate:

MCE 顧客使用本產(chǎn)品發(fā)表的 86 篇科研文獻(xiàn)

WB

    Abemaciclib methanesulfonate purchased from MCE. Usage Cited in: Nature. 2017 Aug 24;548(7668):471-475.  [Abstract]

    Western blot of SKBR3, BT474, MDA-MB-453, and MDA-MB-361 cells treated with DMSO, GW572016, or Abemaciclib for 48?h. Western blot of MDA-MB-453 cells pretreated with DMSO or Abemaciclib (500?nM) for 0, 1, or 7 days before exposure to Staurosporine (500?nM) for 4?h.

    Abemaciclib methanesulfonate purchased from MCE. Usage Cited in: Cancer Res. 2017 May 1;77(9):2488-2499.  [Abstract]

    Treatment with PD 0332991 and Abemaciclib shows an induction of S241 P-PDK1 as early as 1 h after drug exposure without an increased in total PDK1 protein.

    Abemaciclib methanesulfonate purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.

    Abemaciclib methanesulfonate purchased from MCE. Usage Cited in: Biochem Pharmacol. 2017 Jan 15;124:29-42.  [Abstract]

    Effect of LY2835219 on the expression of ABCB1 or ABCG2 in MDR cells. The protein level of ABCB1 and ABCG2 on MDR cells after 0, 0.1, 0.2 and 0.4 μM LY2835219 stimulation for 48h are measured by Western blot analysis, and mRNA level are measured by PCR (GAPDH as loading control).

    Abemaciclib methanesulfonate purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134.  [Abstract]

    Abemaciclib causes increased PARP cleavage in RCC. In 786-O cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with SU 11248.

    Abemaciclib methanesulfonate purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134.  [Abstract]

    Abemaciclib causes increased PARP cleavage in RCC. In Caki-1 cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with SU 11248.

    Abemaciclib methanesulfonate purchased from MCE. Usage Cited in: Oncotarget. 2017 Jun 27;8(40):67422-67438.  [Abstract]

    GTSE1 protein and mRNA levels in MDA-MB-157 and MDA-MB-231 cell lines treated respectively with Abemaciclib 0.5 μM for 24h. Data are presented as mean±SEM of three independent experiments.

    Abemaciclib methanesulfonate purchased from MCE. Usage Cited in: Cancer Res. 2016 Nov 15;76(22):6723-6734.  [Abstract]

    The effects of the CDK inhibitor Abemaciclib, PD 0332991 and Ribocilib on Trop2 ICD cleavage. CDK inhibitors decrease Trop2 ICD abundance after the 2nd day of CDK inhibitor treatment.

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively[1][2][3].

    IC50 & Target[3]

    Cdk4/cyclin D1

    2 nM (IC50)

    CDK6/cyclinD1

    10 nM (IC50)

    CDK9/cyclinT1

    57 nM (IC50)

    CDK5/p35

    287 nM (IC50)

    Cdk5/p25

    355 nM (IC50)

    CDK2/cyclinE

    504 nM (IC50)

    CDK1/cyclinB1

    1627 nM (IC50)

    CDK7/Mat1/cyclinH1

    3910 nM (IC50)

    PIM1

    50 nM (IC50)

    PIM2

    3400 nM (IC50)

    HIPK2

    31 nM (IC50)

    DYRK2

    61 nM (IC50)

    CK2

    117 nM (IC50)

    GSK3b

    192 nM (IC50)

    JNK3

    389 nM (IC50)

    FLT3 (D835Y)

    403 nM (IC50)

    DRAK1

    659 nM (IC50)

    FLT3

    3960 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HCT-116 IC50
    0.54 μM
    Compound: Ly2835219
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    		[PMID: 30165341]
    MCF7 IC50
    0.71 μM
    Compound: Ly2835219
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    		[PMID: 30165341]
    PANC-1 IC50
    5.94 μM
    Compound: Ly2835219
    Antiproliferative activity against human PANC1 cells after 72 hrs by MTT assay
    Antiproliferative activity against human PANC1 cells after 72 hrs by MTT assay
    		[PMID: 30165341]
    體外研究
    (In Vitro)

    Abemaciclib methanesulfonate (LY2835219) 降低細(xì)胞活力，IC50 值范圍為 0.5 μM 至 0.7 μM，抑制頭頸部鱗狀細(xì)胞癌 (HNSCC) 細(xì)胞中的 Akt 和 ERK 信號(hào)但不抑制 mTOR 激活[1]。
    Abemaciclib methanesulfonate (LY2835219) 對(duì) A375R1-4、M14R 和 SH4R 具有抑制作用，EC50 值范圍為 0.3 至 0.6 μM；Abemaciclib methanesulfonate 抑制親本 A375 和耐藥 A375RV1 和 A375RV2 細(xì)胞的增殖，其效力相似，IC50 值分別為 395、260 和 463 nM[2]。
    Abemaciclib methanesulfonate (LY2835219) 以低納摩爾濃度抑制 CDK4 和 CDK6，抑制 Rb 磷酸化，導(dǎo)致 G1 期停滯和增殖抑制，其活性對(duì) Rb 富集細(xì)胞具有特異性[3]。

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

    Abemaciclib methanesulfonate (LY2835219) (45 mg/kg，po) 與 RAD001 聯(lián)合使用在 HNSCC 異種移植腫瘤中產(chǎn)生協(xié)同抗腫瘤作用[1]。
    Abemaciclib methanesulfonate (LY2835219) (45 或 90 mg/kg，口服) 在 A375 異種移植模型中表現(xiàn)出顯著的腫瘤生長(zhǎng)抑制作用[2]。

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

    602.70

    Formula

    C28H36F2N8O3S
    CAS 號(hào)
    性狀

    固體

    顏色

    White to yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    H2O 中的溶解度 : 125 mg/mL (207.40 mM; 超聲助溶)

    DMSO 中的溶解度 : 10 mg/mL (16.59 mM; 超聲助溶 (<80°C); 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 1.6592 mL 8.2960 mL 16.5920 mL
    5 mM 0.3318 mL 1.6592 mL 3.3184 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 (sealed storage, away from moisture)。-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。

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

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

      Solubility: ≥ 2.5 mg/mL (4.15 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。

      以 1 mL 工作液為例，取 100 μL 25.0 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。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (4.15 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(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    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(qǐng)依序添加每種溶劑： PBS

      Solubility: 25 mg/mL (41.48 mM); 澄清溶液; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑： 0.5% Hydroxyethyl cellulose in Water

      Solubility: 12.5 mg/mL (20.74 mM); 澄清溶液; 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)過程有損耗，建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.95%

    參考文獻(xiàn)
    Cell Assay
    [1]

    Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between Abemaciclib (LY2835219) and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of < 1 is synergistic and a CI of > 1 is antagonistic.

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

    Six-week-old BALB/c female nude mice are injected subcutaneously with OSC-19 (1×106) cells. When tumor sizes reach approximately 100 mm3, mice are randomized by tumor size and subjected to each treatment. At least 5 mice per treatment group are included. Each group of mice is dosed via daily oral gavage with vehicle, Abemaciclib (LY2835219) (45 mg/kg/d or 90 mg/kg/d), RAD001 (5 mg/kg/d), or a combination of both. The Abemaciclib (LY2835219) is dissolved in 1% HEC in 20 mM phosphate buffer (pH2.0). Tumor size and body weight are measured twice weekly. Tumor volumes are calculated using the following formula: V=(L × W2)/2 (L, Length; W, width). Mice are gavaged a final time on day 14 and sacrificed the following day. The tumors are removed for Western blot and immunohistochemistry.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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 (sealed storage, away from moisture)。-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 / H2O 1 mM 1.6592 mL 8.2960 mL 16.5920 mL 41.4800 mL
    5 mM 0.3318 mL 1.6592 mL 3.3184 mL 8.2960 mL
    10 mM 0.1659 mL 0.8296 mL 1.6592 mL 4.1480 mL
    15 mM 0.1106 mL 0.5531 mL 1.1061 mL 2.7653 mL
    H2O 20 mM 0.0830 mL 0.4148 mL 0.8296 mL 2.0740 mL
    25 mM 0.0664 mL 0.3318 mL 0.6637 mL 1.6592 mL
    30 mM 0.0553 mL 0.2765 mL 0.5531 mL 1.3827 mL
    40 mM 0.0415 mL 0.2074 mL 0.4148 mL 1.0370 mL
    50 mM 0.0332 mL 0.1659 mL 0.3318 mL 0.8296 mL
    60 mM 0.0277 mL 0.1383 mL 0.2765 mL 0.6913 mL
    80 mM 0.0207 mL 0.1037 mL 0.2074 mL 0.5185 mL
    100 mM 0.0166 mL 0.0830 mL 0.1659 mL 0.4148 mL

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    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：
    Abemaciclib methanesulfonate
    目錄號(hào)：
    HY-16297
    需求量：