Molecular Weight(MW): 602.7
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.
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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.
Biochem J 2014 459(3), 513-24. abemaciclib (LY2835219) purchased from Selleck.
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Choose Selective CDK Inhibitors
|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.|
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. |
|In vitro||Water||100 mg/mL (165.92 mM)|
|DMSO||83 mg/mL (137.71 mM)|
|Ethanol||24 mg/mL (39.82 mM)|
|In vivo||Add solvents individually and in order:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02327143||Completed||Healthy Volunteers||Eli Lilly and Company||January 2015||Phase 1|
|NCT02256267||Completed||Healthy Volunteers||Eli Lilly and Company||October 2014||Phase 1|
|NCT02117648||Completed||Neoplasm|Neoplasm Metastasis||Eli Lilly and Company||April 2014||Phase 1|
|NCT02057133||Recruiting||Breast Neoplasms||Eli Lilly and Company||March 2014||Phase 1|
|NCT02059148||Completed||Healthy Volunteers||Eli Lilly and Company||February 2014||Phase 1|
|NCT02014129||Active, not recruiting||Neoplasm Metastasis|Lymphoma||Eli Lilly and Company||December 2013||Phase 1|
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.
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