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SR-3029

Name: SR-3029
Brand: TargetMol
SKU: T3972
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3972Cas No. 1454585-06-8

Alias SR3029

SR-3029 is a highly potent and specific inhibitor of CK1δ/CK1ε.

SR-3029

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Purity: 99.64%

Catalog No. T3972Alias SR3029Cas No. 1454585-06-8

SR-3029 is a highly potent and specific inhibitor of CK1δ/CK1ε.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
5 mg	$73	In Stock	In Stock
10 mg	$119	In Stock	In Stock
25 mg	$257	In Stock	In Stock
50 mg	$413	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$77	In Stock	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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Batch Information

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Purity:99.64%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

SR-3029 AI Summary

SR-3029 exhibits oral bioavailability in C57BL6 mice with an F value of 13.0%, a half-life of 0.9 hours, an area under the curve (AUC) of 1153.08 ng∙hr/mL, a clearance rate of 49.0 mL/min/kg, and a maximum concentration (Cmax) of 1100.0 nM. It demonstrates significant inhibitory activity against CK1delta with an IC50 of 44.0 nM and CK1epsilon with an IC50 of 260.0 nM, and potent inhibition of CDK13 with an IC50 of 10.0 nM. The compound also displays antiproliferative activity against MDA-MB-231 cells with an EC50 of 26.0 nM and affects cell viability in a cell-type dependent manner, decreasing growth in HEK293T cells but potentially increasing growth in U2OS cells. SR-3029 shows varying aqueous solubility, measured at 100.0 nM at pH 7.4, and affects the thermal stability of protein domains in a domain-specific manner, with Delta TM values ranging from significant increases to slight decreases. It inhibits CYP enzymes in human liver microsomes with a broad range of inhibition percentages (12.0% to 62.0%), except for CYP2D6, which it slightly activates (-3.0%). Moreover, SR-3029 exhibits apparent permeability in PAMPA assays with a Papp value of 0.4 × 10^-6 cm/s, and demonstrates varying half-lives in human, mouse, and rat liver microsomes, indicating its potential for further exploration in the development of CDK-targeted therapies..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	SR-3029 is a highly potent and specific inhibitor of CK1δ/CK1ε.
Targets&IC50	CK1δ:44 nM, CDK4-CyclinD3:368 nM, FLT3:3000 nM, CDK6-CyclinD1:428 nM, CDK6-CyclinD3:427 nM, CK1ε:260 nM, Cdk4-CyclinD1:576 nM
Synonyms	SR3029

Chemical Properties

Molecular Weight	480.45
Formula	C₂₃H₁₉F₃N₈O
Cas No.	1454585-06-8
Smiles	Fc1cccc(c1)-n1cnc2c(NCc3nc4ccc(F)c(F)c4[nH]3)nc(nc12)N1CCOCC1
Relative Density.	1.62 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 45 mg/mL (93.66 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.16 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	2.0814 mL	10.4069 mL	20.8138 mL	104.0691 mL
5 mM	0.4163 mL	2.0814 mL	4.1628 mL	20.8138 mL
10 mM	0.2081 mL	1.0407 mL	2.0814 mL	10.4069 mL
20 mM	0.1041 mL	0.5203 mL	1.0407 mL	5.2035 mL
50 mM	0.0416 mL	0.2081 mL	0.4163 mL	2.0814 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