Atuveciclib (BAY-1143572)

Catalog No.S8727

Atuveciclib (BAY-1143572) Chemical Structure

Molecular Weight(MW): 387.43

Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively.

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Biological Activity

Description Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively.
Targets
CDK9 [1]
(Cell-free assay)
GSK-3α [1]
()
GSK3β [1]
()
13 nM 45 nM 87 nM
In vitro

BAY 1143572 is a potent and highly selective CDK9 inhibitor (IC50 CDK9/CycT1: 13 nM, ratio of IC50 values CDK2/CDK9: 100). Outside the CDK family, submicromolar inhibitory activity was only recorded against GSK3 kinase (IC50 GSK3α: 45 nM, GSK3β: 87 nM). BAY 1143572 demonstrates antiproliferative activity against HeLa cells (IC50 = 920 nM) and MOLM-13 cells (IC50 = 310 nM). It also demonstrates improved Caco-2 permeability and a decreased efflux ratio (PappA→B: 35 nm/s, ER: 6) relative to lead compound BAY‐958 (PappA→B: 22 nm/s, ER: 15)[1].

In vivo

In an in vivo pharmacokinetic study in rats, BAY 1143572 showed low blood clearance (CLb 1.1 L/h/kg). The volumes of distribution (Vss) of BAY 1143572 is 1.0 L/kg. BAY 1143572 shows significantly improved oral bioavailability of 54 %. The blood/plasma ratios is about 1. It does not show significant inhibition of cytochrome P450 activity, with IC50 values >20 μM[1]. The administration of BAY 1143572 in immunocompromized NOD/Shi-scid/IL-2Rγ null (NOG) mice xenografted with patient-derived ATL cells greatly reduced the infiltration of ATL cells into organs, such as liver and bone marrow. Decreased human soluble IL2R levels in serum were also observed, which indicated a reduction of ATL tumor burden[2].

Protocol

Solubility (25°C)

In vitro DMSO 77 mg/mL (198.74 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 387.43
Formula

C18H18FN5O2S

CAS No. 1414943-88-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02345382 Completed Leukemia Bayer February 19 2015 Phase 1
NCT02345382 Completed Leukemia Bayer February 19 2015 Phase 1
NCT01938638 Completed Neoplasms Bayer September 26 2013 Phase 1
NCT01938638 Completed Neoplasms Bayer September 26 2013 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