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Roniciclib

Catalog No. T16784   CAS 1223498-69-8
Synonyms: BAY 1000394

Roniciclib (BAY 1000394) is a potent pan-CDK inhibitor and a novel oral cytotoxic agent. Roniciclib inhibits the activity of cell-cycle CDKs CDK1, CDK2, CDK3, CDK4, and of transcriptional CDKs CDK7 and CDK9 with IC(50) values in the range between 5 and 25 nmol/L.

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Roniciclib Chemical Structure
Roniciclib, CAS 1223498-69-8
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Roniciclib (BAY 1000394) is a potent pan-CDK inhibitor and a novel oral cytotoxic agent. Roniciclib inhibits the activity of cell-cycle CDKs CDK1, CDK2, CDK3, CDK4, and of transcriptional CDKs CDK7 and CDK9 with IC(50) values in the range between 5 and 25 nmol/L.
Targets&IC50 CDK2/CyclinE:9 nM, CDK4/cyclin D:11 nM, CDK9/CyclinT1:5 nM, Cdk1/cyclin B:7 nM, CDK7/Cyclin H/MAT1:25 nM
In vitro Roniciclib inhibits the kinase activity of the cell-cycle CDKs CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclinD (IC50: 7, 9, and 11 nM, respectively). Roniciclibeffectively inhibits the proliferation of various human and murine tumor cell lines with a very balanced profile (mean IC50 on human tumor cells: 16 nM). The transcriptional CDKs CDK9/cyclin T1 and CDK7/cyclin H/MAT1 are inhibited in a similar range (5 and 25 nM) [1][2].
In vivo Roniciclib has low blood clearance rates in mouse, rat, and dog (0.51, 0.78, and 0.50 Lh-1kg-1, respectively). Roniciclib strongly inhibits the growth of HeLa-MaTu tumors that have been grown to a size of approximately 50mm2 before the start of treatment. Roniciclib (1.5 and 1 mg/kg) treatment slow tumor growth to T/C values of 0.15 and 0.62, respectively. The addition of Roniciclib to cisplatin causes a strong tumor growth inhibition with T/C values of 0.01 (1.0 mg/kg Roniciclib) and -0.02 (1.5 mg/kg Roniciclib) [1][2].
Synonyms BAY 1000394
Molecular Weight 430.44
Formula C18H21F3N4O3S
CAS No. 1223498-69-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 249 mg/mL (578.47 mM)

TargetMolReferences and Literature

1. Siemeister G, et al. BAY 1000394, a novel cyclin-dependent kinase inhibitor, with potent antitumor activity in mono- and in combination treatment upon oral application. Mol Cancer Ther. 2012 Oct;11(10):2265-73. 2. Lücking U, et al. The lab oddity prevails: discovery of pan-CDK inhibitor (R)-S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide (BAY 1000394) for the treatment of cancer. ChemMedChem. 2013 Jul;8(7):1067-85.

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Keywords

Roniciclib 1223498-69-8 Cell Cycle/Checkpoint CDK BAY 1000394 Cyclin dependent kinase BAY1000394 BAY-1000394 inhibit Inhibitor inhibitor

 

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