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Abemaciclib mesylate (LY2835219)
Catalog No.S7158
For research use only.
Abemaciclib (LY2835219) 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.
CAS No. 1231930-82-7
Selleck's Abemaciclib mesylate (LY2835219) has been cited by 68 publications
Purity & Quality Control
Choose Selective CDK Inhibitors
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Other CDK Products
Biological Activity
| Description | Abemaciclib (LY2835219) 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. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| Assay |
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| 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)
Solubility (25°C)
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In vitro |
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In vivo |
Add solvents to the product individually and in order |
100mg/mL |
Chemical Information
| Molecular Weight | 602.7 | ||
|---|---|---|---|
| Formula | C27H32F2N8.CH4O3S |
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| CAS No. | 1231930-82-7 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CCN1CCN(CC1)CC2=CN=C(C=C2)NC3=NC=C(C(=N3)C4=CC5=C(C(=C4)F)N=C(N5C(C)C)C)F.CS(=O)(=O)O | ||
In vivo Formulation Calculator (Clear solution)
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT05440786 | Not yet recruiting | Drug: Abemaciclib|Drug: Irinotecan|Drug: Temozolomide | Sarcoma Ewing|Neoplasm Metastasis | Eli Lilly and Company | August 15 2022 | Phase 2 |
| NCT05386108 | Not yet recruiting | Drug: Abemaciclib|Drug: Elacestrant | Breast Neoplasms|Brain Neoplasms|Neoplasms by Site|Neoplasms|Breast Diseases|Central Nervous System Neoplasms|Brain Diseases|Central Nervous System Diseases | Stemline Therapeutics Inc. | August 2022 | Phase 1|Phase 2 |
| NCT04791384 | Recruiting | Drug: Abemaciclib|Drug: Elacestrant | Breast Cancer | Criterium Inc. | April 21 2022 | Phase 1|Phase 2 |
| NCT05169567 | Recruiting | Drug: Abemaciclib|Drug: Fulvestrant|Drug: Placebo | Breast Neoplasm|Neoplasm Metastasis | Eli Lilly and Company | March 11 2022 | Phase 3 |
(data from https://clinicaltrials.gov, updated on 2022-08-01)
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
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Frequently Asked Questions
Question 1:
Is your product S7158 LY2835219 “mesylate salt form”?
Answer:
Our S7158 LY2835219 is mesylate salt form.
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