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

Abemaciclib methanesulfonate  (Synonyms: LY2835219 methanesulfonate)

製品番号: HY-16297 純度: 99.84%
COA 取扱説明書 Technical Support

Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective and BBB-permeable CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively.

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CAS 番号 : 1231930-82-7

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10 mM * 1 mL in DMSO
ready for reconstitution
 USD 80 在庫あり
Solution
10 mM * 1 mL in DMSO USD 80 在庫あり
Solid
5 mg $60 在庫あり
10 mg $90 在庫あり
50 mg $120 在庫あり
100 mg $150 在庫あり
200 mg $190 在庫あり
500 mg $350 在庫あり
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カスタマーレビュー

Based on 117 publication(s) in Google Scholar

Other Forms of Abemaciclib methanesulfonate:

Abemaciclib methanesulfonate 関連抗体

Top Publications Citing Use of Products

顧客検証

In Vivo Efficacy Study
WB
Cell Proliferation/Viability Assay

    Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Nov 21;9(1):373.  [Abstract]

    MCL17-PDX mice were treated as indicated: vehicle (n = 5), abemaciclib (50 mg/kg, oral, daily; n = 5), and volasertib (5 mg/kg, intraperitoneal, weekly; n = 5). Tumor size was measured every 7 days during the treatment. Tumor volume = length x width2/2. Mice were euthanized after 21 days of treatment. Tumors were excised and weighed in comparison between each group.

    Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112.  [Abstract]

    MPF-R and TPF-R cells were treated with different concentrations of the CDK4/6 inhibitor (CDK4/6i) Palbociclib (HY-A0065), Ribociclib (HY-15777C) or Abemaciclib (HY-16297A) for 6 days. Cell growth was measured by crystal violet colorimetric assay. Growth relative to vehicle (%) is plotted against log drug concentration.

    Abemaciclib methanesulfonate purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.

    CDK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective and BBB-permeable 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)

    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    0.54 3
    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]
    HCT-116 IC50
    0.54 3
    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 3
    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]
    MCF7 IC50
    0.71 3
    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]
    HCT-116 IC50
    0.54 3
    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]
    PANC-1 IC50
    5.94 3
    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]
    PANC-1 IC50
    5.94 3
    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]
    MCF7 IC50
    0.71 3
    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 3
    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]
    体外実験

    Abemaciclib (LY2835219) reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells[1].
    Abemaciclib (LY2835219) shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; Abemaciclib inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC50 values of 395, 260, and 463 nM, respectively[2].
    Abemaciclib (LY2835219) inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells[3].

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

    Abemaciclib methanesulfonate 関連抗体
    体内実験

    Abemaciclib (LY2835219) (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor[1].
    Abemaciclib (LY2835219) (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    602.70

    分子式

    C28H36F2N8O3S
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CC(N1C2=CC(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)=CC(F)=C2N=C1C)C.CS(=O)(O)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    H2O : 125 mg/mL (207.40 mM; Need ultrasonic)

    DMSO : 10 mg/mL (16.59 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.1659 mL 0.8296 mL 1.6592 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    ×
    体積 （開始）

    V1

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    濃度 （終了）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (4.15 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 25 mg/mL (41.48 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    純度とドキュメンテーション

    純度: 99.95%

    COA (246 KB) HNMR (146 KB) LCMS (230 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Abemaciclib methanesulfonate Related Classifications

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    Abemaciclib1231930-82-7LY2835219LY 2835219LY-2835219CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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