BAY 1251152

For research use only.

Catalog No.S8730 Synonyms: (+)-BAY-1251152 

BAY 1251152 Chemical Structure

CAS No. 1610358-56-9

BAY1251152 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.

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Biological Activity

Description BAY1251152 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

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]

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]

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: mice and rats with xenograft models (eg. MOLM13)
  • Dosages: --
  • Administration: IV
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 81 mg/mL (200.28 mM)
Water Insoluble
Ethanol 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 404.43
Formula

C19H18F2N4O2S

CAS No. 1610358-56-9
Storage powder
in solvent
Synonyms (+)-BAY-1251152 
Smiles COC1=C(C=CC(=C1)F)C2=CC(=NC=C2F)NC3=NC=CC(=C3)CS(=N)(=O)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02745743 Completed Drug: BAY1251152 Hematologic Neoplasms Bayer June 17 2016 Phase 1
NCT02635672 Active not recruiting Drug: BAY 1251152 Neoplasms Bayer February 10 2016 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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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID