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Roniciclib

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Roniciclib Basic information

Product Name:
Roniciclib
Synonyms:
  • BAY 1000394
  • Roniciclib
  • BAY 1000394 (Roniciclib)
  • BAY1000394 /BAY-1000394
  • Roniciclib (Synonyms: BAY 1000394)
  • Roniciclib (BAY 1000394)
  • 2-Butanol, 3-[[2-[[4-[[S(R)]-S-cyclopropylsulfonimidoyl]phenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]oxy]-, (2R,3R)-
  • (2R,3R)-3-((2-((4-(cyclopropanesulfonimidoyl)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)oxy)butan-2-ol
CAS:
1223498-69-8
MF:
C18H21F3N4O3S
MW:
430.44
Mol File:
1223498-69-8.mol
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Roniciclib Chemical Properties

Boiling point:
577.4±60.0 °C(Predicted)
Density 
1.50±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO: ≥ 250 mg/mL (580.80 mM)
form 
Solid
color 
White to off-white
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Roniciclib Usage And Synthesis

Description

Roniciclib is an orally bioavailable cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. Roniciclib selectively binds to and inhibits the activity of CDK1/Cyclin B, CDK2/Cyclin E, CDK4/Cyclin D1, and CDK9/Cyclin T1, serine/threonine kinases that play key roles in the regulation of the cell cycle progression and cellular proliferation. Inhibition of these kinases leads to cell cycle arrest during the G1/S transition, thereby leading to an induction of apoptosis, and inhibition of tumor cell proliferation. CDKs are often dysregulated in cancerous cells.

Uses

BAY 1000394 (Roniciclib)l is a type I pan-CDK inhibitor which is used in xenograft cancer models. Anticancer agent.

in vivo

Tumor growth is strongly inhibited in a dose-dependent manner with T/C values of 0.19 at the lower dose and of 0.02 (tumor regression) at the higher dose. Furthermore, Roniciclib strongly inhibits growth of HeLa-MaTu tumors that have been grown to a size of approximately 50mm2 before start of treatment (day 8 after inoculation). Treatment with Roniciclib at doses of 1.5 and 1 mg/kg slow tumor growth to T/C values of 0.15 and 0.62, respectively. Addition of Roniciclib to cisplatin result in 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].
Roniciclib has low blood clearance rates in mouse, rat, and dog (0.51, 0.78, and 0.50 Lh-1kg-1, respectively) [2].

IC 50

Cdk1/cyclin B: 7 nM (IC50); CDK2/cyclinE: 9 nM (IC50); CDK4/cyclin D: 11 nM (IC50); CDK9/cyclinT1: 5 nM (IC50); CDK7/Cyclin H/MAT1: 25 nM (IC50)

References

[1] GERHARD SIEMEISTER. BAY 1000394, a novel cyclin-dependent kinase inhibitor, with potent antitumor activity in mono- and in combination treatment upon oral application.[J]. Molecular Cancer Therapeutics, 2012, 11 10: 2265-2273. DOI:10.1158/1535-7163.MCT-12-0286.
[2] DR. ULRICH LÜCKING. 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[J]. ChemMedChem, 2013, 8 7: 1067-1085. DOI:10.1002/cmdc.201300096.

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