Abemaciclib mesylate

Catalog No.S7158 Batch:S715802

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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 83 mg/mL (137.71 mM)
Ethanol 24 mg/mL (39.82 mM)
* <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. [1]
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. [1]

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.

Customer Product Validation

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

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

Selleck's Abemaciclib mesylate has been cited by 83 publications

Intracellular calcium links milk stasis to lysosome-dependent cell death during early mammary gland involution [ Cell Mol Life Sci, 2024, 81(1):29] PubMed: 38212474
mTORC1 activity oscillates throughout the cell cycle promoting mitotic entry and differentially influencing autophagy induction [ bioRxiv, 2024, 2024.02.06.579216] PubMed: 38370755
cGAS-STING drives ageing-related inflammation and neurodegeneration [ Nature, 2023, 620(7973):374-380] PubMed: 37532932
Cyclin E-induced replicative stress drives p53-dependent whole-genome duplication [ Cell, 2023, 186(3):528-542.e14] PubMed: 36681079
Inhibition of CDK4/6 regulates AD pathology, neuroinflammation and cognitive function through DYRK1A/STAT3 signaling [ Pharmacol Res, 2023, 190:106725] PubMed: 36907286
Sequential activation of E2F via Rb degradation and c-Myc drives resistance to CDK4/6 inhibitors in breast cancer [ Cell Rep, 2023, 42(11):113198] PubMed: 37865915
CDK4/6 inhibitors induce replication stress to cause long-term cell cycle withdrawal [ EMBO J, 2022, 10.15252/embj.2021108599] PubMed: 35037284
Clinically relevant CHK1 inhibitors abrogate wild-type and Y537S mutant ERα expression and proliferation in luminal primary and metastatic breast cancer cells [ J Exp Clin Cancer Res, 2022, 41(1):141] PubMed: 35418303
Overexpressed Cyclin D1 and CDK4 proteins are responsible for the resistance to CDK4/6 inhibitor in breast cancer that can be reversed by PI3K/mTOR inhibitors [ Sci China Life Sci, 2022, 10.1007/s11427-021-2140-8] PubMed: 35982377
Implementation of a combined CDK inhibition and arginine-deprivation approach to target arginine-auxotrophic glioblastoma multiforme cells [ Cell Death Dis, 2022, 13(6):555] PubMed: 35717443

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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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