LY2835219 (Abemaciclib) Mesylate

Catalog No.S7158 Batch:S715805

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Technical Data

Formula

C27H32F2N8.CH4O3S
Molecular Weight 602.7 CAS No. 1231930-82-7
Solubility (25°C)* In vitro Water 100 mg/mL (165.92 mM)
DMSO 33 mg/mL (54.75 mM)
Ethanol 4 mg/mL (6.63 mM)
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Abemaciclib mesylate is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.
Targets
CDK4 [1]
(Cell-free assay)		 CDK6 [1]
(Cell-free assay)
2 nM 10 nM
In vitro

LY2835219 is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of the serine/threonine kinases CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.

In vivo

LY2835219 saturates BBB efflux with an unbound plasma IC50 of about 95 nM. The percent of dose in brain for LY2835219-MsOH is 0.5–3.9%. In both a subcutaneous and intracranial human glioblastoma model (U87MG), LY2835219-MsOH suppressed tumor growth in a dose-dependent manner both as a single agent, and in combination with temozolomide.

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    SYO-1 cells

  • Concentrations

    100 nM

  • Incubation Time

    24 h

  • Method

    Cells were cultured overnight and, on the next day (day 1), the media was replaced containing 100nM Abemaciclib or vehicle control (DMSO).
Animal Study:

[3]
  • Animal Models

    Female C57BL/6 mice

  • Dosages

    50 mg/kg

  • Administration

    i.p.

References

  • https://pubmed.ncbi.nlm.nih.gov/29497278/
  • https://pubmed.ncbi.nlm.nih.gov/33495604/
  • https://pubmed.ncbi.nlm.nih.gov/32929370/

Customer Product Validation

<p>HT29 cells were treated with DMSO control, 1 uM selumetinib (Sel), 5 uM PD0332991 (991), 0.3 uM LY2835219 (219) or serum-free (SF) medium for 48 h. Whole cell extracts were prepared, fractionated by SDS/PAGE and analysed by Western blotting with the indicated antibodies.</p>

Data from [ Biochem J , 2014 , 459(3), 513-24 ]

SJSA cells were treated with the alternate CDK4/6 inhibitors Ribociclib (LEE011) and Abemaciclib (LY2835219) for 30 h, alone or in combination with Nutlin at 20 µM for 6 h. Immunoblot analysis was performed as in (a). Like Palbociclib (PD0332991), the combination of Nutlin with alternate CDK4/6 inhibitors diminished p53 target gene expression when compared to Nutlin treatment alone.

Data from [ , , Cell Death Dis, 2018, 9(9):918 ]

Selleck's LY2835219 (Abemaciclib) Mesylate Has Been Cited by 97 Publications

eIF4A Inhibitors Suppress Cell-Cycle Feedback Response and Acquired Resistance to CDK4/6 Inhibition in Cancer [ Molecular Cancer Therapeutics, November 1, 2019, 2158-2170] PubMed: 31395685
Inhibition of ACAA1 Restrains Proliferation and Potentiates the Response to CDK4/6 Inhibitors in Triple-Negative Breast Cancer [ Cancer Research, May 15, 2023, 1711-1724] PubMed: 37129951
Inhibition of CDK4/6 regulates AD pathology, neuroinflammation and cognitive function through DYRK1A/STAT3 signaling [ Pharmacological Research, March 11, 2023, 106725] PubMed: 36907286
Clinical CDK4/6 inhibitors induce selective and immediate dissociation of p21 from cyclin D-CDK4 to inhibit CDK2 [ Nature Communications, June 7, 2021, 3356] PubMed: 34099663
Phenotype-based probabilistic analysis of heterogeneous responses to cancer drugs and their combination efficacy [ PLoS Computational Biology, February 21, 2020, e1007688] PubMed: 32084135
Combined therapy with DR5-targeting antibody-drug conjugate and CDK inhibitors as a strategy for advanced colorectal cancer [ Cell Rep Med, 2025, S2666-3791(25)00231-9] PubMed: 40449480
A bedside-to-bench translational analysis of NF1 alterations and CDK4/6 inhibitor resistance in hormone receptor-positive metastatic breast cancer [ EBioMedicine, 2025, 118:105828] PubMed: 40578027
MUC1-C dependency in drug resistant HR+/HER2- breast cancer identifies a new target for antibody-drug conjugate treatment [ NPJ Breast Cancer, 2025, 11(1):39] PubMed: 40287441
ACSL4 promotes the formation of the proliferative subtype in hepatoblastoma [ BMC Cancer, 2025, 25(1):191] PubMed: 39901207
SLC7A11 protects luminal A breast cancer cells against ferroptosis induced by CDK4/6 inhibitors [ Redox Biol, 2024, 76:103304] PubMed: 39153252

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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