abemaciclib mesylate (LY2835219)

Catalog No.S7158

abemaciclib mesylate (LY2835219) Chemical Structure

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 mesylate (LY2835219) purchased from Selleck.

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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.
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells  NUDaR5JNTnWwY4Tpc44h[XO|YYm= M2X1VVUxKG2rboO= NFvzWG9Ed22yZYTpeIl3\SCrbnjpZol1cW:wIH;mJIh2dWGwIFPET|Qw[3mlbHnuJGQyKGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMh[XO|ZYPz[YQh[XNicHjvd5Bpd3K7bHH0bY9vKG:oIFPUVmYh[W[2ZYKgOVAhdWmwczDifUBOcWOqYXXsbZMuVWWwdHXuJJBtd3RiYX7hcJl{cXNiaX6gdJJme2WwY3Wgc4YhSVSSLDDLbV0xNjZibl2= NEOyR5ozPjFzNUW3NS=>
insect cells  MnHHSpVv[3Srb36gZZN{[Xl? NF7hcpc2OCCvaX7z MWDJcohq[mm2aX;uJI9nKGi3bXHuJGNFUzRxY4njcIlvKERzIHX4dJJme3OnZDDpckBqdnOnY4SgZ4VtdHNiYYPz[ZN{\WRiYYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGNVWkZiYX\0[ZIhPTBibXnud{BjgSCvaXPyc5Bt[XSnIIPjbY51cWyuYYTpc44h[2:3boTldkwhUUN3ME2yJI5O NHLxXWszPjFzNUW3NS=>
human COLO205 cells M3PZT2Z2dmO2aX;uJIF{e2G7 MUmyOEBp MUfJcohq[mm2aX;uJI9nKEOGS{SvOkBqdiCqdX3hckBEV0yRMkC1JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiUnKgdIhwe3Cqb4L5cIF1cW:wIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIxie2W{LYPjZY5vcW6pIH\seY9z\XOlZX7j[UBucWO{b4DsZZRmKGO7dH;t[ZRzcWNiYX7hcJl{cXN? MVuyOlEyPTV5MR?=
human COLO205 cells NE\JdYNHfW6ldHnvckBie3OjeR?= MUiyOEBp MVXJcohq[mm2aX;uJI9nKEOGS{SvOkBqdiCqdX3hckBEV0yRMkC1JINmdGy|IHHzd4V{e2WmIHHzJI1igGmvdX2gZ4VtdCCleXPs[UBienKnc4SgZZQhTzFicHjhd4Uh[W[2ZYKgNlQhcHK|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnzve{BkgXSxbXX0dolkKGGwYXz5d4l{ NXiyWlhDOjZzMUW1O|E>

... Click to View More Cell Line Experimental Data

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]


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)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.

* 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


CAS No. 1231930-82-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02919696 Active not recruiting Advanced Cancer|Metastatic Cancer Eli Lilly and Company August 7 2017 Phase 1
NCT01394016 Active not recruiting Advanced Cancer Eli Lilly and Company December 7 2009 Phase 1
NCT02763566 Active not recruiting Breast Cancer Eli Lilly and Company December 5 2016 Phase 3
NCT03703466 Not yet recruiting Metastatic Breast Cancer Eli Lilly and Company October 30 2018 Phase 2
NCT02079636 Active not recruiting Carcinoma Non-small Cell Lung Eli Lilly and Company|Merck Sharp & Dohme Corp. March 28 2014 Phase 1
NCT02675231 Active not recruiting Hormone Receptor Positive Tumor|HER-2 Positive Breast Cancer Eli Lilly and Company May 23 2016 Phase 2

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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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Frequently Asked Questions

  • Question 1:

    Is your product S7158 LY2835219 “mesylate salt form”?

  • Answer:

    Our S7158 LY2835219 is mesylate salt form.

CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID