abemaciclib (LY2835219)

Catalog No.S7158

abemaciclib (LY2835219) Chemical Structure

Molecular Weight(MW): 602.7

1 Customer Review

  • 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.

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description 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.
Targets
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  MWjGeY5kfGmxbjDhd5NigQ>? MoTVOVAhdWmwcx?= Mlr6R49ueGW2aYTpeoUhcW6qaXLpeIlwdiCxZjDoeY1idiCFRFu0M4N6[2yrbjDENUBmgHC{ZYPz[YQhcW5iaX7z[YN1KGOnbHzzJIF{e2W|c3XkJIF{KHCqb4PwbI9zgWyjdHnvckBw\iCFVGLGJIFnfGW{IEWwJI1qdnNiYomgUYlkcGGnbHnzMW1mdnSnbjDwcI91KGGwYXz5d4l{KGmwIIDy[ZNmdmOnIH;mJGFVWCxiS3m9NE43KG6P Mo[xNlYyOTV3N{G=
insect cells  MYnGeY5kfGmxbjDhd5NigQ>? MknyOVAhdWmwcx?= MoXQTY5pcWKrdHnvckBw\iCqdX3hckBETEt2L3P5Z4xqdiCGMTDlfJBz\XO|ZXSgbY4hcW6|ZXP0JINmdGy|IHHzd4V{e2WmIHHzJJBpd3OyaH;yfYxifGmxbjDv[kBEXFKIIHHmeIVzKDVyIH3pcpMh[nlibXnjdo9xdGG2ZTDzZ4lvfGmubHH0bY9vKGOxdX70[ZItKEmFNUC9NkBvVQ>? Mn7BNlYyOTV3N{G=
human COLO205 cells MnPqSpVv[3Srb36gZZN{[Xl? MUGyOEBp NH7P[YZKdmirYnn0bY9vKG:oIFPET|QwPiCrbjDoeY1idiCFT1zPNlA2KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gVoIheGixc4Doc5J6dGG2aX;uJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKGyjc3XyMZNk[W6waX7nJIZtfW:{ZYPj[Y5k\SCvaXPyc5Bt[XSnIHP5eI9u\XS{aXOgZY5idHm|aYO= NXHXT|V1OjZzMUW1O|E>
human COLO205 cells MWDGeY5kfGmxbjDhd5NigQ>? NUDY[GNsOjRiaB?= NHHyOVRKdmirYnn0bY9vKG:oIFPET|QwPiCrbjDoeY1idiCFT1zPNlA2KGOnbHzzJIF{e2W|c3XkJIF{KG2jeHnteY0h[2WubDDjfYNt\SCjcoLld5Qh[XRiR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[oxwfyCleYTvcYV1emmlIHHuZYx6e2m| Mmj4NlYyOTV3N{G=

... 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]

Protocol

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 water 100mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
Formula

C27H32F2N8.CH4O3S

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

Bio Calculators

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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

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID