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SY-5609

Name: SY-5609
Brand: TargetMol
SKU: T36038
Price: 583 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T36038Cas No. 2417302-07-7

Alias CDK7-IN-3

SY-5609 (CDK7-IN-3) is a selective non-covalent CDK7 inhibitor (Kd value is 0.07 nM), with weak inhibitory activity against CDK2, CDK9 and CDK12 with IC50 values of 5.5, 1.9 and 1.7 μM, respectively, and has anti-tumor activity and inhibits cell apoptosis.

SY-5609

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Purity: 99.94%

Catalog No. T36038Alias CDK7-IN-3Cas No. 2417302-07-7

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$142	In Stock	In Stock
2 mg	$211	In Stock	In Stock
5 mg	$361	In Stock	In Stock
10 mg	$583	In Stock	In Stock
25 mg	Preferential	In Stock	In Stock
50 mg	Preferential	-	In Stock
1 mL x 10 mM (in DMSO)	$392	In Stock	In Stock

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

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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:99.94%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	SY-5609 (CDK7-IN-3) is a selective non-covalent CDK7 inhibitor (Kd value is 0.07 nM), with weak inhibitory activity against CDK2, CDK9 and CDK12 with IC50 values of 5.5, 1.9 and 1.7 μM, respectively, and has anti-tumor activity and inhibits cell apoptosis.
Targets&IC50	CDK12:870 nM (Ki), CDK7:0.065 nM (Kd), CDK9:960 nM (Ki), CDK2:2600 nM (Ki)
In vitro	METHODS: HCC70 cells were treated with SY-5609 （CDK7-IN-3） (25, 50, 100, 250, 500 nM), and protein samples were collected at 6, 24 and 48 h after treatment. Immunoblotting was used to detect the protein levels of Phospho-CDK2 T160, total CDK2, c-MYC, MCL1, cyclinB1, RNAPII Ser5 phosphorylation and total RNAPII; HCC70, MDA-MB-468, CAOV3, OVCAR3 and HDF cells were treated with SY-5609 （CDK7-IN-3） (100, 250, 500 nM) for 48 and 72 h, and Annexin V-FITC and propidium iodide (PI) were used to detect cell apoptosis. RESULTS Treatment of HCC70 cells with SY-5609 （CDK7-IN-3） for 24 and 48 hours inhibited phosphorylation of CDK2 at Thr160 by loss of CAK function; inhibition of CDK7 in TFIIH resulted in reduced phosphorylation of Ser5 in the C-terminal heptad repeat of RNA polymerase II and decreased cMyc levels; SY-5609 （CDK7-IN-3） treatment resulted in a mild reduction in MCL1 protein only at 48 h; SY-5609 （CDK7-IN-3） induced apoptosis and cell cycle arrest at G2/M in multiple cancer cell lines at 48 and 72 h, as detected by Annexin V/PI staining, but not in primary fibroblast cell lines. [1]
In vivo	METHODS: SY-5609 (CDK7-IN-3) (2 mg/kg, orally, once daily, for 21 days) was administered to HCC70 cell line-derived xenograft models, and tumor volume and body weight were measured twice weekly. One-tailed t test was used to evaluate the significance of the anti-tumor effect of SY-5609 (CDK7-IN-3). RESULTS The plasma exposure in mice treated with SY-5609 (CDK7-IN-3) was 261.28 ng h/mL, Cmax was 50.67 ng/mL (103 nM), and the elimination half-life was 3.33 h. During the 21-day dosing period, the tumor regressed and was well tolerated, with no tumor regrowth on day 28. [1]
Synonyms	CDK7-IN-3

Chemical Properties

Molecular Weight	490.46
Formula	C₂₃H₂₆F₃N₆OP
Cas No.	2417302-07-7
Smiles	C(F)(F)(F)C=1C(C=2C=3C(NC2)=C(P(C)(C)=O)C(C#N)=CC3)=NC(N[C@H]4CCC(C)(C)NC4)=NC1

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 16.7 mg/mL (34.05 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.08 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	2.0389 mL	10.1945 mL	20.3890 mL	101.9451 mL
5 mM	0.4078 mL	2.0389 mL	4.0778 mL	20.3890 mL
10 mM	0.2039 mL	1.0195 mL	2.0389 mL	10.1945 mL
20 mM	0.1019 mL	0.5097 mL	1.0195 mL	5.0973 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