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Roniciclib

Chemical Structure : Roniciclib

CAS No.: 1223498-69-8

Roniciclib (BAY 10-00394;BAY 1000394)

Catalog No.: PC-61246Not For Human Use, Lab Use Only.

Roniciclib (BAY 1000394) is a potent, orally active, pan-CDK inhibitor with IC50 of 7/9/11 nM for CDK1/2/4 respectively, inhibits transcriptional CDK9/7 with IC50 of 5-25 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Roniciclib (BAY 1000394) is a potent, orally active, pan-CDK inhibitor with IC50 of 7/9/11 nM for CDK1/2/4 respectively, inhibits transcriptional CDK9/7 with IC50 of 5-25 nM.
BAY1000394 inhibits 16 additional kinase in a panel of 214 non-CDK Ser/Thr and Tyr kinases.
BAY1000394 simultaneously inhibits cell-cycle progression and RNA polymerase II-mediated gene transcription, shows broad and uniform inhibitory activity on cell proliferation with IC50 of 8-33 nM.
BAY1000394 potently inhibits growth of various human tumor xenografts.

Physicochemical Properties

M.Wt 430.44
Formula C18H21F3N4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-S-Cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide

References

1. Siemeister G, et al. Mol Cancer Ther. 2012 Oct;11(10):2265-73.

2. Lücking U, et al. ChemMedChem. 2013 Jul;8(7):1067-85.

3. Ayaz P, et al. ACS Chem Biol. 2016 Jun 17;11(6):1710-9.

4. Bahleda R, et al. Br J Cancer. 2017 Jun 6;116(12):1505-1512.

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