1. Cell Cycle/DNA Damage
  2. CDK

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

Cat. No.: HY-16297 Purity: 99.87%
Data Sheet SDS 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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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: 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.
    • 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

    IC50: 2 nM (CDK4), 10 nM (CDK6)

    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
    NCT Number Sponsor Condition Start Date Phase
    NCT02482935 Eli Lilly and Company Healthy June 2015 Phase 1
    NCT02981940 Dana-Farber Cancer Institute|Eli Lilly and Company Glioblastoma February 9, 2017 Phase 2
    NCT03130439 Dana-Farber Cancer Institute|Eli Lilly and Company Breast Cancer May 26, 2017 Phase 2
    NCT02846987 Memorial Sloan Kettering Cancer Center|Eli Lilly and Company Sarcoma|Dedifferentiated Liposarcoma July 2016 Phase 2
    NCT02919696 Eli Lilly and Company Advanced Cancer|Metastatic Cancer July 2017 Phase 1
    NCT02411591 Eli Lilly and Company Carcinoma, Non-Small-Cell Lung|Neoplasm Metastasis June 2015 Phase 1
    NCT02387814 Eli Lilly and Company Hepatic Insufficiency|Healthy March 2015 Phase 1
    NCT03220646 Memorial Sloan Kettering Cancer Center|Eli Lilly and Company Brain Tumor July 13, 2017 Phase 2
    NCT02831530 Gustave Roussy, Cancer Campus, Grand Paris Breast Cancer March 2016 Phase 2
    NCT02644460 Emory University Diffuse Intrinsic Pontine Glioma|Brain Tumor, Recurrent|Solid Tumor, Recurrent|Neuroblastoma, Recurrent, Refractory|Ewing Sarcoma, Recurrent, Refractory|Rhabdomyosarcoma, Recurrent, Refractory|Osteosarcoma, Recurrent, Refractory|Rhabdoid Tumor, Recurrent, Refractory February 2016 Phase 1
    NCT02677844 Eli Lilly and Company Healthy February 2016 Phase 1
    NCT02672423 Eli Lilly and Company Healthy February 2016 Phase 1
    NCT02450539 Eli Lilly and Company Non-Small Cell Lung Cancer Stage IV August 2015 Phase 2
    NCT02152631 Eli Lilly and Company Non Small Cell Lung Cancer September 2014 Phase 3
    NCT03155997 Eli Lilly and Company Breast Cancer July 12, 2017 Phase 3
    NCT02688088 Eli Lilly and Company Neoplasm Metastasis February 2016 Phase 1
    NCT02747004 Eli Lilly and Company Metastatic Breast Cancer September 2016 Phase 2
    NCT02441946 Eli Lilly and Company Breast Cancer|Hormone Receptor Positive Tumor|Early-Stage Breast Carcinoma August 2015 Phase 2
    NCT02308020 Eli Lilly and Company Breast Cancer|Non-small Cell Lung Cancer|Melanoma|Brain Metastases April 2015 Phase 2
    NCT02107703 Eli Lilly and Company Breast Neoplasms July 2014 Phase 3
    NCT02102490 Eli Lilly and Company Metastatic Breast Cancer June 2014 Phase 2
    NCT02779751 Eli Lilly and Company|Merck Sharp & Dohme Corp. Non Small Cell Lung Cancer|Breast Cancer November 14, 2016 Phase 1
    NCT02675231 Eli Lilly and Company Hormone Receptor Positive Tumor|HER-2 Positive Breast Cancer March 2016 Phase 2
    NCT02884089 Eli Lilly and Company Healthy August 2016 Phase 1
    NCT02981342 Eli Lilly and Company Pancreatic Ductal Adenocarcinoma January 2017 Phase 2
    NCT02763566 Eli Lilly and Company Breast Cancer December 2016 Phase 3
    NCT02792725 Eli Lilly and Company Metastatic Breast Cancer
    NCT02246621 Eli Lilly and Company Breast Cancer November 2014 Phase 3
    NCT03099174 Boehringer Ingelheim Neoplasms|Breast Neoplasms May 4, 2017 Phase 1
    NCT02079636 Eli Lilly and Company|Merck Sharp & Dohme Corp. Carcinoma, Non-small Cell Lung March 2014 Phase 1
    NCT02745769 Eli Lilly and Company Advanced Cancer|Colorectal Cancer|Mantle Cell Lymphoma October 2016 Phase 1
    NCT02977780 Dana-Farber Cancer Institute|Eli Lilly and Company|Celgene|Puma Biotechnology, Inc.|Accelerate Brain Cancer Cure Glioblastoma February 9, 2017 Phase 2
    NCT02857270 Eli Lilly and Company Advanced Cancer|Metastatic Melanoma|Metastatic Non-small Cell Lung Cancer|Metastatic Pancreatic Ductal Adenocarcinoma|Colorectal Cancer September 2016 Phase 1
    NCT02791334 Eli Lilly and Company Solid Tumor|Microsatellite Instability-High (MSI-H) Solid Tumors|Cutaneous Melanoma June 29, 2016 Phase 1
    NCT02784795 Eli Lilly and Company Solid Tumor|Breast Cancer|Colon Cancer|Cholangiocarcinoma|Soft Tissue Sarcoma November 2016 Phase 1
    NCT02482935 Eli Lilly and Company Healthy June 2015 Phase 1
    NCT02981940 Dana-Farber Cancer Institute|Eli Lilly and Company Glioblastoma February 9, 2017 Phase 2
    NCT03130439 Dana-Farber Cancer Institute|Eli Lilly and Company Breast Cancer May 26, 2017 Phase 2
    NCT02846987 Memorial Sloan Kettering Cancer Center|Eli Lilly and Company Sarcoma|Dedifferentiated Liposarcoma July 2016 Phase 2
    NCT02919696 Eli Lilly and Company Advanced Cancer|Metastatic Cancer July 2017 Phase 1
    NCT02411591 Eli Lilly and Company Carcinoma, Non-Small-Cell Lung|Neoplasm Metastasis June 2015 Phase 1
    NCT02387814 Eli Lilly and Company Hepatic Insufficiency|Healthy March 2015 Phase 1
    NCT03220646 Memorial Sloan Kettering Cancer Center|Eli Lilly and Company Brain Tumor July 13, 2017 Phase 2
    NCT02831530 Gustave Roussy, Cancer Campus, Grand Paris Breast Cancer March 2016 Phase 2
    NCT02644460 Emory University Diffuse Intrinsic Pontine Glioma|Brain Tumor, Recurrent|Solid Tumor, Recurrent|Neuroblastoma, Recurrent, Refractory|Ewing Sarcoma, Recurrent, Refractory|Rhabdomyosarcoma, Recurrent, Refractory|Osteosarcoma, Recurrent, Refractory|Rhabdoid Tumor, Recurrent, Refractory February 2016 Phase 1
    NCT02677844 Eli Lilly and Company Healthy February 2016 Phase 1
    NCT02672423 Eli Lilly and Company Healthy February 2016 Phase 1
    NCT02450539 Eli Lilly and Company Non-Small Cell Lung Cancer Stage IV August 2015 Phase 2
    NCT02152631 Eli Lilly and Company Non Small Cell Lung Cancer September 2014 Phase 3
    NCT03155997 Eli Lilly and Company Breast Cancer July 12, 2017 Phase 3
    NCT02688088 Eli Lilly and Company Neoplasm Metastasis February 2016 Phase 1
    NCT02747004 Eli Lilly and Company Metastatic Breast Cancer September 2016 Phase 2
    NCT02441946 Eli Lilly and Company Breast Cancer|Hormone Receptor Positive Tumor|Early-Stage Breast Carcinoma August 2015 Phase 2
    NCT02308020 Eli Lilly and Company Breast Cancer|Non-small Cell Lung Cancer|Melanoma|Brain Metastases April 2015 Phase 2
    NCT02107703 Eli Lilly and Company Breast Neoplasms July 2014 Phase 3
    NCT02102490 Eli Lilly and Company Metastatic Breast Cancer June 2014 Phase 2
    NCT02779751 Eli Lilly and Company|Merck Sharp & Dohme Corp. Non Small Cell Lung Cancer|Breast Cancer November 14, 2016 Phase 1
    NCT02675231 Eli Lilly and Company Hormone Receptor Positive Tumor|HER-2 Positive Breast Cancer March 2016 Phase 2
    NCT02884089 Eli Lilly and Company Healthy August 2016 Phase 1
    NCT02981342 Eli Lilly and Company Pancreatic Ductal Adenocarcinoma January 2017 Phase 2
    NCT02763566 Eli Lilly and Company Breast Cancer December 2016 Phase 3
    NCT02792725 Eli Lilly and Company Metastatic Breast Cancer
    NCT02246621 Eli Lilly and Company Breast Cancer November 2014 Phase 3
    NCT03099174 Boehringer Ingelheim Neoplasms|Breast Neoplasms May 4, 2017 Phase 1
    NCT02079636 Eli Lilly and Company|Merck Sharp & Dohme Corp. Carcinoma, Non-small Cell Lung March 2014 Phase 1
    NCT02745769 Eli Lilly and Company Advanced Cancer|Colorectal Cancer|Mantle Cell Lymphoma October 2016 Phase 1
    NCT02977780 Dana-Farber Cancer Institute|Eli Lilly and Company|Celgene|Puma Biotechnology, Inc.|Accelerate Brain Cancer Cure Glioblastoma February 9, 2017 Phase 2
    NCT02857270 Eli Lilly and Company Advanced Cancer|Metastatic Melanoma|Metastatic Non-small Cell Lung Cancer|Metastatic Pancreatic Ductal Adenocarcinoma|Colorectal Cancer September 2016 Phase 1
    NCT02791334 Eli Lilly and Company Solid Tumor|Microsatellite Instability-High (MSI-H) Solid Tumors|Cutaneous Melanoma June 29, 2016 Phase 1
    NCT02784795 Eli Lilly and Company Solid Tumor|Breast Cancer|Colon Cancer|Cholangiocarcinoma|Soft Tissue Sarcoma November 2016 Phase 1
    NCT02482935 Eli Lilly and Company Healthy June 2015 Phase 1
    NCT02981940 Dana-Farber Cancer Institute|Eli Lilly and Company Glioblastoma February 9, 2017 Phase 2
    NCT03130439 Dana-Farber Cancer Institute|Eli Lilly and Company Breast Cancer May 26, 2017 Phase 2
    NCT02846987 Memorial Sloan Kettering Cancer Center|Eli Lilly and Company Sarcoma|Dedifferentiated Liposarcoma July 2016 Phase 2
    NCT02919696 Eli Lilly and Company Advanced Cancer|Metastatic Cancer July 2017 Phase 1
    NCT02411591 Eli Lilly and Company Carcinoma, Non-Small-Cell Lung|Neoplasm Metastasis June 2015 Phase 1
    NCT02387814 Eli Lilly and Company Hepatic Insufficiency|Healthy March 2015 Phase 1
    NCT03220646 Memorial Sloan Kettering Cancer Center|Eli Lilly and Company Brain Tumor July 13, 2017 Phase 2
    NCT02831530 Gustave Roussy, Cancer Campus, Grand Paris Breast Cancer March 2016 Phase 2
    NCT02644460 Emory University Diffuse Intrinsic Pontine Glioma|Brain Tumor, Recurrent|Solid Tumor, Recurrent|Neuroblastoma, Recurrent, Refractory|Ewing Sarcoma, Recurrent, Refractory|Rhabdomyosarcoma, Recurrent, Refractory|Osteosarcoma, Recurrent, Refractory|Rhabdoid Tumor, Recurrent, Refractory February 2016 Phase 1
    NCT02677844 Eli Lilly and Company Healthy February 2016 Phase 1
    NCT02672423 Eli Lilly and Company Healthy February 2016 Phase 1
    NCT02450539 Eli Lilly and Company Non-Small Cell Lung Cancer Stage IV August 2015 Phase 2
    NCT02152631 Eli Lilly and Company Non Small Cell Lung Cancer September 2014 Phase 3
    NCT03155997 Eli Lilly and Company Breast Cancer July 12, 2017 Phase 3
    NCT02688088 Eli Lilly and Company Neoplasm Metastasis February 2016 Phase 1
    NCT02747004 Eli Lilly and Company Metastatic Breast Cancer September 2016 Phase 2
    NCT02441946 Eli Lilly and Company Breast Cancer|Hormone Receptor Positive Tumor|Early-Stage Breast Carcinoma August 2015 Phase 2
    NCT02308020 Eli Lilly and Company Breast Cancer|Non-small Cell Lung Cancer|Melanoma|Brain Metastases April 2015 Phase 2
    NCT02107703 Eli Lilly and Company Breast Neoplasms July 2014 Phase 3
    NCT02102490 Eli Lilly and Company Metastatic Breast Cancer June 2014 Phase 2
    NCT02779751 Eli Lilly and Company|Merck Sharp & Dohme Corp. Non Small Cell Lung Cancer|Breast Cancer November 14, 2016 Phase 1
    NCT02675231 Eli Lilly and Company Hormone Receptor Positive Tumor|HER-2 Positive Breast Cancer March 2016 Phase 2
    NCT02884089 Eli Lilly and Company Healthy August 2016 Phase 1
    NCT02981342 Eli Lilly and Company Pancreatic Ductal Adenocarcinoma January 2017 Phase 2
    NCT02763566 Eli Lilly and Company Breast Cancer December 2016 Phase 3
    NCT02792725 Eli Lilly and Company Metastatic Breast Cancer
    NCT02246621 Eli Lilly and Company Breast Cancer November 2014 Phase 3
    NCT03099174 Boehringer Ingelheim Neoplasms|Breast Neoplasms May 4, 2017 Phase 1
    NCT02079636 Eli Lilly and Company|Merck Sharp & Dohme Corp. Carcinoma, Non-small Cell Lung March 2014 Phase 1
    NCT02745769 Eli Lilly and Company Advanced Cancer|Colorectal Cancer|Mantle Cell Lymphoma October 2016 Phase 1
    NCT02977780 Dana-Farber Cancer Institute|Eli Lilly and Company|Celgene|Puma Biotechnology, Inc.|Accelerate Brain Cancer Cure Glioblastoma February 9, 2017 Phase 2
    NCT02857270 Eli Lilly and Company Advanced Cancer|Metastatic Melanoma|Metastatic Non-small Cell Lung Cancer|Metastatic Pancreatic Ductal Adenocarcinoma|Colorectal Cancer September 2016 Phase 1
    NCT02791334 Eli Lilly and Company Solid Tumor|Microsatellite Instability-High (MSI-H) Solid Tumors|Cutaneous Melanoma June 29, 2016 Phase 1
    NCT02784795 Eli Lilly and Company Solid Tumor|Breast Cancer|Colon Cancer|Cholangiocarcinoma|Soft Tissue Sarcoma November 2016 Phase 1
    NCT02014129 Eli Lilly and Company Neoplasm Metastasis|Lymphoma December 2013 Phase 1
    NCT02327143 Eli Lilly and Company Healthy Volunteers January 2015 Phase 1
    NCT02059148 Eli Lilly and Company Healthy Volunteers February 2014 Phase 1
    NCT02117648 Eli Lilly and Company Neoplasm|Neoplasm Metastasis April 2014 Phase 1
    NCT01913314 Eli Lilly and Company Healthy Volunteers August 2013 Phase 1
    NCT02256267 Eli Lilly and Company Healthy Volunteers October 2014 Phase 1
    NCT01739309 Eli Lilly and Company Mantle Cell Lymphoma March 2013 Phase 2
    NCT01394016 Eli Lilly and Company Advanced Cancer December 7, 2009 Phase 1
    NCT02057133 Eli Lilly and Company Breast Neoplasms March 10, 2014 Phase 1
    View MoreCollapse
    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]

    LY2835219 is dissolved in DMSO to a 10 mM concentration. 

    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]

    LY2835219 is dissolved in 1% HEC in 20 mM phosphate buffer.

    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

    602.7

    Formula

    C₂₈H₃₆F₂N₈O₃S

    CAS No.

    1231930-82-7

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    H2O: ≥ 250 mg/mL

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

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.87%

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