Abemaciclib mesylate (LY2835219)
For research use only.
Catalog No.S7158
44 publications

CAS No. 1231930-82-7
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.
Purity & Quality Control
Choose Selective CDK Inhibitors
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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Targets |
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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
Solubility (25°C)
In vitro | Water | 100 mg/mL (165.92 mM) |
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DMSO | 83 mg/mL (137.71 mM) | |
Ethanol | '''24 mg/mL | |
In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): water For best results, use promptly after mixing. |
100mg/mL |
* 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.
Chemical Information
Molecular Weight | 602.7 |
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Formula | C27H32F2N8.CH4O3S |
CAS No. | 1231930-82-7 |
Storage |
powder in solvent |
Synonyms | N/A |
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)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
Dosage | mg/kg | Average weight of animals | g | Dosing volume per animal | ul | Number of animals | ||||
Step 2: Enter the in vivo formulation () | ||||||||||
% DMSO % % Tween 80 % ddH2O | ||||||||||
CalculateReset |
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: : mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL,)
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.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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NCT04627064 | Not yet recruiting | Drug: Abemaciclib|Drug: MK-6482 | Clear Cell Renal Cell Carcinoma | Dana-Farber Cancer Institute|Eli Lilly and Company | March 2021 | Phase 1 |
NCT04169074 | Not yet recruiting | Drug: Abemaciclib|Drug: Abemaciclib plus nivolumab | HNSCC | University of Arizona | January 1 2021 | Phase 2 |
NCT04408924 | Not yet recruiting | Drug: Abemaciclib | Metastatic Castration-Resistant Prostate Cancer | Eli Lilly and Company | December 18 2020 | Phase 2 |
NCT04238819 | Recruiting | Drug: Abemaciclib|Drug: Irinotecan|Drug: Temozolomide | Relapsed Solid Tumor|Refractory Solid Tumor | Eli Lilly and Company | November 9 2020 | Phase 1 |
NCT04514159 | Recruiting | Drug: ZN-c5|Drug: Abemaciclib | Breast Cancer | Zeno Alpha Inc. | November 2020 | Phase 1 |
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
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Question 1:
Is your product S7158 LY2835219 “mesylate salt form”?
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Answer:
Our S7158 LY2835219 is mesylate salt form.