Home Cell Cycle CDK inhibitor Enitociclib (BAY 1251152) For research use only.

Enitociclib (BAY 1251152)

Synonyms: (+)-BAY-1251152 

Enitociclib (BAY 1251152) is a potent PTEFb/CDK9 inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins.

Enitociclib (BAY 1251152) Chemical Structure

Enitociclib (BAY 1251152) Chemical Structure

CAS: 1610358-56-9

Selleck's Enitociclib (BAY 1251152) has been cited by 6 publications

Purity & Quality Control

Batch: S873001 DMSO] 81 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.87%
99.87

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Signaling Pathway

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CDK Signaling Pathway

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Biological Activity

Description Enitociclib (BAY 1251152) is a potent PTEFb/CDK9 inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins.
Targets
CDK9 [2]
(Cell-free assay)
3 nM
In vitro
In vitro

BAY 1251152 (compound 2) significantly inhibits CDK9 and CDK2 with IC50 of 3 nM and 360 nM, respectively. BAY 1251152 (compound 2) shows cellular potency in MOLM13 with IC50 of 29 nM.[1] [2]
Cell Research Cell lines HeLa, NCI-H460, A2780, DU 145, HeLa-MaTu-ADR, Caco-2, B16F10, MOLM-13
Concentrations 0.001 μM - 10 μM
Incubation Time 4 days
Method

Cultivated tumour cells are plated in a 96-well multititer plate in 200 of their respective growth medium supplemented 10% fetal calf serum. After 24 hours, the cells of one plate (zero-point plate) are stained with crystal violet, while the medium of the other plates is replaced by fresh culture medium (200 μl ), to which the test substances are added in various concentrations (0 μM, as well as in the range of 0.001 -10 μM; the final concentration of the solvent dimethyl sulfoxide is 0.5%). The cells are incubated for 4 days in the presence of test substances.
In Vivo
In vivo

BAY 1251152 demonstrates excellent efficacy upon i.v. treatment in xenograft models (e.g. MOLM13) in mice and rats. BAY 1251152 is currently being evaluated in Phase I studies to determine the safety, tolerability, pharmacokinetics and initial pharmacodynamic biomarker response in patients with advanced cancer.[2]
Animal Research Animal Models mice and rats with xenograft models (eg. MOLM13)
Dosages --
Administration IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02745743 Completed
Hematologic Neoplasms
Bayer
 June 17 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 404.43 Formula

C19H18F2N4O2S
CAS No. 1610358-56-9 SDF --
Smiles COC1=C(C=CC(=C1)F)C2=CC(=NC=C2F)NC3=NC=CC(=C3)CS(=N)(=O)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 81 mg/mL ( (200.28 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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