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Roniciclib

Name: Roniciclib
Brand: TargetMol
SKU: T16784
Price: 55 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16784Cas No. 1223498-69-8

Alias 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.

Roniciclib

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Purity: 98.63%

Catalog No. T16784Alias BAY 1000394Cas No. 1223498-69-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$55	In Stock	In Stock
5 mg	$127	In Stock	In Stock
10 mg	$186	In Stock	In Stock
25 mg	$312	In Stock	In Stock
50 mg	$488	In Stock	In Stock
100 mg	$846	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.63%

Color:White

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

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	CDK7-CyclinH-MAT1:25 nM, CDK1-CyclinB:7 nM, CDK4-CyclinD:11 nM, CDK2-CyclinE:9 nM, CDK9-CyclinT1:5 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

Chemical Properties

Molecular Weight	430.44
Formula	C₁₈H₂₁F₃N₄O₃S
Cas No.	1223498-69-8
Smiles	C[C@@H](O)[C@@H](C)Oc1nc(Nc2ccc(cc2)[S@](=N)(=O)C2CC2)ncc1C(F)(F)F
Relative Density.	1.50 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 249 mg/mL (578.48 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.62 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3232 mL	11.6160 mL	23.2320 mL	116.1602 mL
5 mM	0.4646 mL	2.3232 mL	4.6464 mL	23.2320 mL
10 mM	0.2323 mL	1.1616 mL	2.3232 mL	11.6160 mL
20 mM	0.1162 mL	0.5808 mL	1.1616 mL	5.8080 mL
50 mM	0.0465 mL	0.2323 mL	0.4646 mL	2.3232 mL
100 mM	0.0232 mL	0.1162 mL	0.2323 mL	1.1616 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc