Home Cell Cycle CDK inhibitor Enitociclib (BAY 1251152)

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Enitociclib (BAY 1251152) CDK inhibitor

Cat.No.S8730

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. It 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) CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 404.43

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 404.43 Formula

C19H18F2N4O2S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1610358-56-9 -- Storage of Stock Solutions

Synonyms (+)-BAY-1251152  Smiles COC1=C(C=CC(=C1)F)C2=CC(=NC=C2F)NC3=NC=CC(=C3)CS(=N)(=O)C

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
CDK9 [2]
(Cell-free assay)
3 nM
In vitro

Enitociclib (BAY 1251152) (compound 2) significantly inhibits CDK9 and CDK2 with IC50 of 3 nM and 360 nM, respectively, and shows cellular potency in MOLM13 with IC50 of 29 nM.[1] [2]
In vivo

Enitociclib (BAY 1251152) demonstrates excellent efficacy upon i.v. treatment in xenograft models (e.g. MOLM13) in mice and rats. It 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]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02745743 Completed
Hematologic Neoplasms
Bayer
 June 17 2016 Phase 1

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