1. Cell Cycle/DNA Damage
  2. CDK

LY2835219 (Synonyms: ABEMACICLIB; CDK4/6 dual inhibitor)

Cat. No.: HY-16297 Purity: 99.87%
Handling Instructions

LY2835219 a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

For research use only. We do not sell to patients.

LY2835219 Chemical Structure

LY2835219 Chemical Structure

CAS No. : 1231930-82-7

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Estimated Time of Arrival: December 31
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Customer Review

Other Forms of LY2835219:

    LY2835219 purchased from MCE. Usage Cited in: Cancer Res. 2016 Nov 15;76(22):6723-6734.

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

    LY2835219 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2017 Jan 15;124:29-42.

    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).

    LY2835219 purchased from MCE. Usage Cited in: Cancer Res. 2017 May 1;77(9):2488-2499.

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

    LY2835219 purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.

    Effects of Palbociclib on CDK4/6-Rb pathway. HCC cells are treated with different doses of Palbociclib for 24 h, and then, the cells are subjected to western blot analysis.

    LY2835219 purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.

    Inhibition of AMPK reverses Palbociclib-induced autophagy and apoptosis. Hep3B cells are incubated with AMPK inhibitor (Compound C, 2.5 μM) for 4 h and then treated with Palbociclib for 24 h. Apoptotic cells are determined by flow cytometry.

    LY2835219 purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.

    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.

    LY2835219 purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.

    Co-treatment of Metformin and Ribociclib induces cell death in Hep3B cells. Cells are exposed to Ribociclib at 25 μM and/or Metformin at 10 mM for 72 h.

    LY2835219 purchased from MCE. Usage Cited in: Nature. 2017 Aug 24;548(7668):471-475.

    Western blot of SKBR3, BT474, MDA-MB-453, and MDA-MB-361 cells treated with DMSO, Lapatinib, 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.

    LY2835219 purchased from MCE. Usage Cited in: Oncotarget. 2017 Jun 27;8(40):67422-67438.

    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.

    LY2835219 purchased from MCE. Usage Cited in: Mol Cell. 2017 Oct 19;68(2):336-349.e6.

    AMPK DKO SV40-immortalized MEFs are electroporated with plasmids encoding Myc-tagged AMPK α1, Myc-tagged AMPK α2 and Myc-tagged AMPK α2 S > A. 48 hr later, MEFs are starved for 3 hr and treated for 2 hr with DMSO or 50 mM A769662 before protein extraction. Western blot analysis shows the A769662-induced ACC phosphorylation in transfected cells.

    LY2835219 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363.

    LAPC-4 cells are grown in charcoal-stripped serum medium (CSS) for 24 hours and then stimulated by R1881 alone or with different doses of Palbociclib (PD). Palbociclib is added 30 min before androgen treatment. Cellular expression of all proteins is detected by immunoblotting analysis. β-actin is included as a control for protein loading.

    LY2835219 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363.

    LAPC-4 cells are grown in charcoal-stripped serum medium (CSS) for 24 hours and then stimulated by R1881 alone or with different doses of LDC000067. LDC000067 is added 30 min before androgen treatment. Cellular expression of all proteins was detected by immunoblotting analysis. β-actin was included as a control for protein loading.

    LY2835219 purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134.

    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 Sunitinib.

    LY2835219 purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134.

    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 Sunitinib.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    LY2835219 a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

    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)

    In Vitro

    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]. LY2835219 shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; LY2835219 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]. 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].

    In Vivo

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

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 250 mg/mL (414.80 mM)

    *"≥" means soluble, but saturation unknown.

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      LY2835219 is dissolved in 1% HEC in 20 mM phosphate buffer (pH2.0) and administered orally by gavage (final volume 0.2 mL)[4].

    References
    Kinase Assay
    [1]

    Cells (5 × 103) are plated in 96 well plates. Cells are treated the next day for 24 to 48 hours and then assessed for caspase-3 activity by Caspase-Glo-3/7 Assay, as per manufacturer's instructions and a luminescence plate reader.

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

    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 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, LY2835219 (45 mg/kg/d or 90 mg/kg/d), Everolimus (5 mg/kg/d), or a combination of both. The 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.

    References
    Molecular Weight

    602.70

    Formula

    C₂₈H₃₆F₂N₈O₃S

    CAS No.

    1231930-82-7

    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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.87%

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    Product Name:
    LY2835219
    Cat. No.:
    HY-16297
    Quantity:

    LY2835219

    Cat. No.: HY-16297