Home Cell Cycle CDK inhibitor Abemaciclib mesylate For research use only.

Abemaciclib mesylate

Synonyms: LY2835219 mesylate

Abemaciclib mesylate 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.

Abemaciclib mesylate Chemical Structure

Abemaciclib mesylate Chemical Structure

CAS No. 1231930-82-7

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Abemaciclib mesylate Related Products

Signaling Pathway

CDK Signaling Pathways

CDK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human COLO205 cells Function assay 24 h Inhibition of CDK4/6 in human COLO205 cells assessed as maximum cell cycle arrest at G1 phase after 24 hrs by propidium iodide staining-based flow cytometric analysis 26115571
human COLO205 cells Function assay 24 h Inhibition of CDK4/6 in human COLO205 cells assessed as inhibition of Rb phosphorylation after 24 hrs by propidium iodide staining-based laser-scanning fluorescence microplate cytometric analysis 26115571
insect cells  Function assay 50 mins Inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by microplate scintillation counter, IC50=2 nM 26115571
insect cells  Function assay 50 mins Competitive inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by Michaelis-Menten plot analysis in presence of ATP, Ki=0.6 nM 26115571
HCT116 Antiproliferative assay 72 hrs IC50 = 0.54 μM 30165341
MCF7 Antiproliferative assay 72 hrs IC50 = 0.71 μM 30165341
PANC1 Antiproliferative assay 72 hrs IC50 = 5.94 μM 30165341
Sf9 Function assay Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP, IC50 = 0.371 μM. 26741853
Sf9 Function assay 90 mins Inhibition of recombinant human N-terminal GST-tagged CDK4 (4 to 303 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintillation countin, Ki = 0.002 μM. 27171036
Sf9 Function assay 90 mins Inhibition of recombinant full length human N-terminal GST-tagged CDK6 (1 to 326 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintilla, Ki = 0.01 μM. 27171036
Sf21 Function assay Inhibition of recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 substrate peptide, Ki = 3.91 μM. 27171036
COLO205 Antiproliferative assay 96 hrs Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay, IC50 = 0.46 μM. 29074254
U87MG Antiproliferative assay 72 hrs Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay, IC50 = 0.0481 μM. 29247857
Sf9 Function assay Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method, IC50 = 0.002 μM. 29429832
Sf9 Function assay 90 mins Inhibition of recombinant human full length CDK6 expressed in baculovirus infected Sf9 insect cells using histone H1 substrate after 90 mins by ADP-Glo assay, IC50 = 0.0078 μM. 29429832
Sf9 Function assay Inhibition of recombinant human N-terminal GST-tagged CDK4 (M1 to A326 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method, IC50 = 0.01 μM. 29429832
Sf9 Function assay 90 mins Inhibition of recombinant human full length CDK1/Cyclin D3 expressed in baculovirus infected Sf9 insect cells using histone H1 substrate after 90 mins by ADP-Glo assay, IC50 = 0.056 μM. 29429832
MDA-MB-231 Antiproliferative activity against human 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay, IC50 = 0.191 μM. 29429832
COLO205 Antiproliferative activity against human 96 hrs Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay, IC50 = 0.217 μM. 29459274
MDA-MB-468 Antiproliferative activity against human 96 hrs Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay, IC50 = 4.808 μM. 29459274
COLO205 Inhibition of CDK4 in human 0.1 to 10 uM 24 hrs Inhibition of CDK4 in human COLO205 cells assessed as reduction in total Rb protein level at 0.1 to 10 uM after 24 hrs by immunoblotting method 29459274
COLO205 Cell cycle assay up to 10 uM 24 hrs Cell cycle arrest in human COLO205 cells assessed as accumulation at G2/M phase up to 10 uM after 24 hrs by propidium iodide staining based FACS analysis 29459274
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Biological Activity

Description Abemaciclib mesylate 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
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 Research Cell lines SYO-1 cells
Concentrations 100 nM
Incubation Time 24 h
Method

Cells were cultured overnight and, on the next day (day 1), the media was replaced containing 100nM Abemaciclib or vehicle control (DMSO).
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Rb(S780) / Rb / p21 p-ERK / ERK / p-Akt / Akt / p-mTOR(S2448) / mTOR pRb(S795) / E2F1 / Cyclin A2 / Cyclin E2 26909611
Growth inhibition assay Cell viability 26909611
In Vivo
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]
Animal Research Animal Models Female C57BL/6 mice
Dosages 50 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06139107 Recruiting
Breast Cancer
Mridula George MD|Rutgers The State University of New Jersey
 June 21 2024 Phase 1
NCT06259929 Not yet recruiting
Breast Cancer
Fondazione Oncotech
 April 1 2024 Phase 2

Chemical Information & Solubility

Molecular Weight 602.7 Formula

C27H32F2N8.CH4O3S
CAS No. 1231930-82-7 SDF Download Abemaciclib mesylate SDF
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
Storage (From the date of receipt)

In vitro
Batch:

Water : 100 mg/mL

DMSO : 24 mg/mL ( (39.82 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 13 mg/mL


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Tech Support

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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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