Atuveciclib (BAY-1143572)

Catalog No.S8727 Batch:S872701

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Technical Data

Formula

C18H18FN5O2S
Molecular Weight 387.43 CAS No. 1414943-88-6
Solubility (25°C)* In vitro DMSO 77 mg/mL (198.74 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.85mg/ml Taking the 1 mL working solution as an example, add 50 μL of 77 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.64mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Atuveciclib (BAY-1143572) is a 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 (from reference)

Selleck's Atuveciclib (BAY-1143572) has been cited by 6 publications

Cyclin-Dependent kinase 9 (CDK9) inhibitor Atuveciclib ameliorates Imiquimod-Induced Psoriasis-Like dermatitis in mice by inhibiting various inflammation factors via STAT3 signaling pathway [ Int Immunopharmacol, 2024, 129:111652] PubMed: 38335657
The methyltransferase METTL3 negatively regulates nonalcoholic steatohepatitis (NASH) progression [ Nat Commun, 2021, 12(1):7213] PubMed: 34893641
Synthesis and Evaluation of a 3, 4‐dihydro‐2H‐benzoxazine Derivative as a Potent CDK9 Inhibitor for Anticancer Therapy [ Bulletin of the Korean Chemical Society, 2021, 42(3):416-419] PubMed: None
Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors [ Cell Chem Biol, 2020, S2451-9456(20)30380-9] PubMed: 33086052
Cyclin-Dependent Kinase 9 (CDK9) Inhibitor Atuveciclib Suppresses Intervertebral Disk Degeneration via the Inhibition of the NF-κB Signaling Pathway [ Front Cell Dev Biol, 2020, 8:579658] PubMed: 33015073
Rational combination therapy for melanoma with dinaciclib by targeting BAK-dependent cell death. [ Mol Cancer Ther, 2019, 10.1158/1535-7163.MCT-19-0451] PubMed: 31744894

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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