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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 64 publications
Purity & Quality Control
Choose Selective CDK Inhibitors
Related Compound Libraries
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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| 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 (from reference)
Solubility (25°C)
|
In vitro |
Water |
100 mg/mL
(165.92 mM) |
| DMSO |
83 mg/mL
(137.71 mM) |
|
| Ethanol |
'''24 mg/mL
|
|
|
In vivo |
Add solvents to the product individually and in order |
100mg/mL |
Chemical Information
| Molecular Weight | 602.7 | ||
|---|---|---|---|
| Formula | C27H32F2N8.CH4O3S |
||
| 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)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
mg/kg
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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.
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.
Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT05169567 | Not yet recruiting | Drug: Abemaciclib|Drug: Fulvestrant|Drug: Placebo | Breast Neoplasm|Neoplasm Metastasis | Eli Lilly and Company | January 14 2022 | Phase 3 |
| NCT04791384 | Not yet recruiting | Drug: Abemaciclib|Drug: Elacestrant | Breast Cancer | Criterium Inc. | January 1 2022 | Phase 1|Phase 2 |
| NCT04967521 | Recruiting | Drug: Abemaciclib|Drug: Placebo | Advanced Dedifferentiated Liposarcoma | Sarcoma Alliance for Research through Collaboration|Eli Lilly and Company | November 11 2021 | Phase 3 |
| NCT04750928 | Recruiting | Drug: Abemaciclib | Neurofibromatosis 1 | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | November 29 2021 | Phase 1|Phase 2 |
| NCT04941274 | Recruiting | Drug: Abemaciclib | Kaposi Sarcoma | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | September 29 2021 | Phase 1|Phase 2 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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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