1. Cell Cycle/DNA Damage
  2. CDK

Roniciclib (Synonyms: BAY 1000394)

Cat. No.: HY-13914
Handling Instructions

Roniciclib is an orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor, with IC50s of 5-25 nM for CDK1, CDK2, CDK3, CDK4, CDK7 and CDK9.

For research use only. We do not sell to patients.

Roniciclib Chemical Structure

Roniciclib Chemical Structure

CAS No. : 1223498-69-8

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Description

Roniciclib is an orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor, with IC50s of 5-25 nM for CDK1, CDK2, CDK3, CDK4, CDK7 and CDK9.

IC50 & Target[1]

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)

In Vitro

Roniciclib (BAY 1000394) inhibits the kinase activity of the cell-cycle CDKs CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclinDwith IC50 values of 7, 9, and 11 nM, respectively. The transcriptional CDKs CDK9/cyclin T1 and CDK7/cyclin H/MAT1 are inhibited in a similar range (5 and 25 nM)[1]. Roniciclib potently inhibits the proliferation of various human and murine tumor cell lines with a very balanced profile (mean IC50 on human tumor cells: 16 nM)[2].

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3232 mL 11.6160 mL 23.2320 mL
5 mM 0.4646 mL 2.3232 mL 4.6464 mL
10 mM 0.2323 mL 1.1616 mL 2.3232 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
Athymic mice bearing established HeLa-MaTu xenograft tumors of approx. 25 mm2 in size are treated orally with Roniciclib (BAY 1000394) at doses of 0.5, 1.0, 1.5, and 2.0 mg/kg once daily for 21 days. Treatment is well tolerated as no body weight loss below the initial body weight is observed. Additional groups of mice are treated on a cyclic intermittent dosing schedule at doses of 1.5, 2.0, and 2.5 mg/kg twice daily for 2 days followed by 5 days without treatment (2 on/5 off). In total, 3 treatment cycles are completed[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

430.44

Formula

C₁₈H₂₁F₃N₄O₃S

CAS No.

1223498-69-8

SMILES

C[[email protected]@H](O)[[email protected]](OC1=NC(NC2=CC=C([[email protected]@](=N)(C3CC3)=O)C=C2)=NC=C1C(F)(F)F)C

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Roniciclib
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Roniciclib

Cat. No.: HY-13914