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GSK215

Name: GSK215
Brand: TargetMol
SKU: T67843
Price: 127 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T67843Cas No. 2743427-26-9

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4), designed using the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase, capable of inducing rapid and prolonged FAK degradation.

GSK215

🥰Excellent

Purity: 99.3%

Catalog No. T67843Cas No. 2743427-26-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$127	In Stock	In Stock
5 mg	$317	In Stock	In Stock
10 mg	$497	In Stock	In Stock
25 mg	$829	In Stock	In Stock
50 mg	$1,150	In Stock	In Stock
100 mg	$1,550	-	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:99.3%

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4), designed using the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase, capable of inducing rapid and prolonged FAK degradation.
In vitro	GSK215 induced degradation is proteasome and ubiquitin dependent. GSK215 (0.1-1000 nM; 2 h) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM in A549 cells[1]. GSK215 (100 nM, 48 h) inhibits migration, invasion and collagen deposition in A549 cells. GSK215 (above 100 nM, 6h) reduces primarily kinases CDK7, RPS6KA3, MET and GAK[1].
In vivo	GSK215 (8 mg/kg; i.h.; once) degrades FAK, and exhibits the Cmax and tmax values of 526 ng/mL and 0.33 hours, respectively[1].

Chemical Properties

Molecular Weight	985.13
Formula	C₅₀H₅₉F₃N₁₀O₆S
Cas No.	2743427-26-9
Smiles	CNC(=O)c1ccccc1Nc1cc(Nc2ccc(cc2OC)N2CCN(CC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(cc3)-c3scnc3C)C(C)(C)C)CC2)ncc1C(F)(F)F
Relative Density.	1.317 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: 225.0 mg/mL (228.4 mM ), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (5.08 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	1.0151 mL	5.0755 mL	10.1509 mL	50.7547 mL
5 mM	0.2030 mL	1.0151 mL	2.0302 mL	10.1509 mL
10 mM	0.1015 mL	0.5075 mL	1.0151 mL	5.0755 mL
20 mM	0.0508 mL	0.2538 mL	0.5075 mL	2.5377 mL
50 mM	0.0203 mL	0.1015 mL	0.2030 mL	1.0151 mL
100 mM	0.0102 mL	0.0508 mL	0.1015 mL	0.5075 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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