Abemaciclib

Catalog No.S5716 Synonyms: LY2835219

Abemaciclib Chemical Structure

Molecular Weight(MW): 506.59

Abemaciclib is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.

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Biological Activity

Description Abemaciclib is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.
Targets
CDK4 [1]
(Cell-free assay)
CDK6 [1]
(Cell-free assay)
2 nM 10 nM
In vitro

Abemaciclib highly selective inhibits the complexes CDK4/ cyclin D1 (IC50 =2 nmol/L) and CDK6/cyclin D1 (IC50 =10 nmol/L), with no activity against other CDK/cyclin complexes or cell-cycle-related kinases within the nanomolar ranges, except for inhibition of CDK9 at IC50 at least five times higher. Besides the cell-cycle dependent activity, abemaciclib is able to boost antitumor immunity by potentiating tumor antigen presentation and selectively suppressing proliferation of regulatory T (Treg) cells at the same time[1]. Consistent with its activity against CDK4 and CDK6, abemaciclib inhibits RB phosphorylation and leads to G1 arrest in RB-proficient cell lines[2]. In vitro, treatment with abemaciclib resulted in increased activation of human T cells and upregulated expression of antigen presentation genes in MCF-7 breast cancer cells[3].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COLO205 cells M3jY[mZ2dmO2aX;uJIF{e2G7 M{DjPVI1KGh? MYjJcohq[mm2aX;uJI9nKEOGS{SvOkBqdiCqdX3hckBEV0yRMkC1JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiUnKgdIhwe3Cqb4L5cIF1cW:wIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIxie2W{LYPjZY5vcW6pIH\seY9z\XOlZX7j[UBucWO{b4DsZZRmKGO7dH;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:OC5zMjFOwG0> M13DclI3OTF3NUex
SK-ES-1 NHzWco5Rem:uaX\ldoF1cW:wIHHzd4F6 NEfnZlk6PiCqb4Xydy=> MVjhcpRqeHKxbHnm[ZJifGm4ZTDl[oZm[3S|IIfpeIgh[W5iYXLzc4x2fGViRVO1NEB3[Wy3ZTDi[YxwfyBzIN88cY9tN0x? NGT4XpQ{ODF|MUO4Oi=>
Cado-ES-1 MYrQdo9tcW[ncnH0bY9vKGG|c3H5 M2O0flk3KGixdYLz M{PZfoFvfGmycn;sbYZmemG2aY\lJIVn\mWldIOge4l1cCCjbjDhZpNwdHW2ZTDFR|UxKH[jbIXlJIJmdG:5IEGg{txud2xxTB?= Ml3SN|AyOzF|OE[=
ES-7 Mme5VJJwdGmoZYLheIlwdiCjc4PhfS=> MXq5OkBpd3W{cx?= MYfhcpRqeHKxbHnm[ZJifGm4ZTDl[oZm[3S|IIfpeIgh[W5iYXLzc4x2fGViRVO1NEB3[Wy3ZTDi[YxwfyBzIN88cY9tN0x? MUOzNFE{OTN6Nh?=
TC-71 MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 M{Dhc|k3KGixdYLz Mn;oZY51cXC{b3zp[oVz[XSrdnWg[YZn\WO2czD3bZRpKGGwIHHid49tfXSnIFXDOVAhfmGudXWgZoVtd3diMTFOwI1wdC:O Mn;uN|AyOzF|OE[=
A673 MoXIVJJwdGmoZYLheIlwdiCjc4PhfS=> MmfqPVYhcG:3coO= NYnBbJpi[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{B4cXSqIHHuJIFje2:udYTlJGVEPTBidnHseYUh[mWub4egNUDPxG2xbD;M M3zyWVMxOTNzM{i2
RD-ES NYLTeZV4WHKxbHnm[ZJifGmxbjDhd5NigQ>? MUC5OkBpd3W{cx?= M4HUSoFvfGmycn;sbYZmemG2aY\lJIVn\mWldIOge4l1cCCjbjDhZpNwdHW2ZTDFR|UxKH[jbIXlJIJmdG:5IEGg{txud2xxTB?= NYmyZY94OzBzM{GzPFY>
ES-1 M2LxTHBzd2yrZnXyZZRqd25iYYPzZZk> MYi5OkBpd3W{cx?= M4\5O4FvfGmycn;sbYZmemG2aY\lJIVn\mWldIOge4l1cCCjbjDhZpNwdHW2ZTDFR|UxKH[jbIXlJIJmdG:5IEGg{txud2xxTB?= NEjSVnU{ODF|MUO4Oi=>
ES-3 MWDQdo9tcW[ncnH0bY9vKGG|c3H5 NE\I[oU6PiCqb4Xydy=> NWrxXXRn[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{B4cXSqIHHuJIFje2:udYTlJGVEPTBidnHseYUh[mWub4egNUDPxG2xbD;M NYXZbWg1OzBzM{GzPFY>
CHLA-258 M{iyNXBzd2yrZnXyZZRqd25iYYPzZZk> NFrGWpE6PiCqb4Xydy=> MkfLZY51cXC{b3zp[oVz[XSrdnWg[YZn\WO2czD3bZRpKGGwIHHid49tfXSnIFXDOVAhfmGudXWgZoVtd3diMTFOwI1wdC:O NEjt[Ik{ODF|MUO4Oi=>
MHH-ES-1 MX3Qdo9tcW[ncnH0bY9vKGG|c3H5 M1Puelk3KGixdYLz NYTNd21j[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{B4cXSqIHHuJIFje2:udYTlJGVEPTBidnHseYUh[mWub4egNUDPxG2xbD;M MU[zNFE{OTN6Nh?=
ES-8 MlTmVJJwdGmoZYLheIlwdiCjc4PhfS=> NWDQ[GU{QTZiaH;1dpM> MXPhcpRqeHKxbHnm[ZJifGm4ZTDl[oZm[3S|IIfpeIgh[W5iYXLzc4x2fGViRVO1NEB3[Wy3ZTDi[YxwfyBzIN88cY9tN0x? MYizNFE{OTN6Nh?=
EW8 NVqzdGh4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NXfWOWFNQTZiaH;1dpM> NGLreoxidnSrcILvcIln\XKjdHn2[UBm\m[nY4TzJJdqfGhiYX6gZYJ{d2y3dHWgSWM2OCC4YXz1[UBj\WyxdzCxJO69dW:uL1y= NWXyOJF[OzBzM{GzPFY>
ES-6 NXjqTZdLWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmTvPVYhcG:3coO= Mlm1ZY51cXC{b3zp[oVz[XSrdnWg[YZn\WO2czD3bZRpKGGwIHHid49tfXSnIFXDOVAhfmGudXWgZoVtd3diMTFOwI1wdC:O M3[xb|MxOTNzM{i2
ES-2 MlnZVJJwdGmoZYLheIlwdiCjc4PhfS=> MVK5OkBpd3W{cx?= MVjhcpRqeHKxbHnm[ZJifGm4ZTDl[oZm[3S|IIfpeIgh[W5iYXLzc4x2fGViRVO1NEB3[Wy3ZTDi[YxwfyBzIN88cY9tN0x? NFzLTZA{ODF|MUO4Oi=>
SMS-CTR MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 MknyPVYhcG:3coO= NWHXcVlO[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{B4cXSqIHHuJIFje2:udYTlJGVEPTBidnHseYUh[mWub4egNUDPxG2xbD;M MY[zNFE{OTN6Nh?=
ES-4 MlfzVJJwdGmoZYLheIlwdiCjc4PhfS=> NXrJeIZrQTZiaH;1dpM> M4XUUYFvfGmycn;sbYZmemG2aY\lJIVn\mWldIOge4l1cCCjbjDhZpNwdHW2ZTDFR|UxKH[jbIXlJIJmdG:5IEGg{txud2xxTB?= M1XqT|MxOTNzM{i2
CT26 NYDXTVA{S2WubDD2bYFjcWyrdImgZZN{[Xl? NEHGTHA6PiCqb4Xydy=> M3[wWGlEPTB;Mj63JO69VQ>? NUjId5hCOjl3M{m0NlU>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CDK6 / CDK4 / AXL ; 

PubMed: 29133594     


MIB/AP WB of H2228 cells treated with abemaciclib or DMSO for 1 hr. 

GSK3β / CAMKII pan ; 

PubMed: 29133594     


MIB/AP WB validation of GSK3β and CAMKIIβ/δ/γ following abemaciclib treatment of H2228 cells. 

β-catenin ; 

PubMed: 29133594     


D-E. Evaluation of β-catenin levels by WB analysis after 6 hr treatment of DMSO, abemaciclib (0.1–10 μM), palbociclib (0.1–10 μM), 1 μM CHIR-99021, or recombinant WNT3A (rWNT3A, 200 ng/ml) in RKO B/R cells (D) or murine L-cells (E). F-G. Evaluation of β-catenin levels by WB analysis of RKO B/R cells (F) or L-cells (G) following treatment with DMSO, 5 μM abemaciclib, 5 μM CHIR-99021, or 10 μM palbociclib over a 30 min – 6 hr time course.

p-Rb / Rb / p-EGFR / EGFR / p-HER2 / HER2 / p-HER3 / HER3 / p-P70S6K / P70S6K / p-S6RP / S6RP / Cyclin D1; 

PubMed: 26977878     


MDA-MB-453 and MDA-MB-361 cells were treated with lapatinib and/or abemaciclib for 24 hours and cell lysates were probed with the antibodies shown.

29133594 26977878
In vivo In a colorectal cancer xenograft model used to develop an integrated pharmacokinetic/pharmacodynamic model, abemaciclib can be dosed orally on a continuous schedule to achieve sustained target inhibition and demonstrates not only durable cell-cycle inhibition but also single-agent antitumor activity. Tumor growth inhibition is observed in multiple other human cancer xenograft models, including those derived from non-small cell lung cancer (NSCLC), melanoma, glioblastoma, and mantle cell lymphoma. Abemaciclib distributes across the blood–brain barrier and prolongs survival in an intracranial glioblastoma xenograft model. In human, The pharmacokinetics of abemaciclib shows a slow absorption phase with a median time from oral dose to maximum plasma concentration (tmax) ranging from 4 to 6 hours. It is extensively cleared and distributed. The mean terminal elimination half-life (t1/2) ranged from 17.4 to 38.1 hours with no apparent dose-dependent change in clearance[2].

Protocol

Cell Research:

[3]

- Collapse
  • Cell lines: CT26 tumor cell line
  • Concentrations: 0-10 μM
  • Incubation Time: 96 h
  • Method:

    Tumor cells were cultured for 4 hr alone at 37°C, and then abemaciclib, palbociclib, or DMSO control was added at indicated concentrations for 96 hr at 37°C. Cell viability was then assessed.


    (Only for Reference)
Animal Research:

[2]

- Collapse
  • Animal Models: Athymic nude mice implanted with human NSCLC xenograft tumors
  • Formulation: 1% HEC
  • Dosages: 25, 50, or 100 mg/kg/d
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 8 mg/mL (15.79 mM)
DMSO 6 mg/mL (11.84 mM)
Water 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 506.59
Formula

C27H32F2N8

CAS No. 1231929-97-7
Storage powder
in solvent
Synonyms LY2835219

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04030728 Not yet recruiting -- Metastatic Breast Cancer|Advanced Breast Cancer Onco Medical Consult GmbH|Eli Lilly and Company|Institut für Frauengesundheit GmbH September 2019 --
NCT03905889 Suspended Drug: Abemaciclib|Drug: Sunitinib Renal Cell Carcinoma Metastatic Milton S. Hershey Medical Center|Eli Lilly and Company June 5 2019 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID