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GSK2008607
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Catalog No. T27454Cas No. 1244644-50-5
GSK2008607 is a potent B-RafV600E inhibitor with anticancer activity and can be used to study breast, colorectal, melanoma, thyroid, and ovarian cancers.
GSK2008607
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Purity: 99.99%
Catalog No. T27454Cas No. 1244644-50-5
GSK2008607 is a potent B-RafV600E inhibitor with anticancer activity and can be used to study breast, colorectal, melanoma, thyroid, and ovarian cancers.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $350 | In Stock | In Stock | |
| 5 mg | $828 | In Stock | In Stock | |
| 10 mg | $1,130 | In Stock | In Stock | |
| 25 mg | $1,590 | In Stock | In Stock | |
| 50 mg | $1,980 | In Stock | In Stock | |
| 100 mg | $2,500 | In Stock | In Stock | |
| 500 mg | $4,900 | - | 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.
Batch Information
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Purity:99.99%
Appearance:Solid
Color:Yellow
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Product Introduction
GSK2008607 AI Summary
GSK2008607 demonstrates significant bioactivity across multiple assays and species. It exhibits intrinsic clearance in rat liver microsomes at a rate of 10.0 mL.min-1.g-1. The compound shows potent antiproliferative activity against human SK-MEL-28 cells expressing the B-Raf V600E mutant, with an EC50 of 8.0 nM after 3 days. Additionally, it effectively inhibits ERK phosphorylation in these cells with an EC50 of 11.0 nM after 1 hour and directly inhibits the B-Raf V600E mutant with an IC50 of 0.5 nM.
In pharmacokinetic studies, GSK2008607 has high oral bioavailability in rats (85.0%), but much lower bioavailability in monkeys (5.0%) and dogs (10.0%). The dose-normalized AUC values are significantly higher in rats (1748.0 ng.hr/ml/mg/kg) compared to monkeys (23.0 ng.hr/ml/mg/kg) and dogs (42.0 ng.hr/ml/mg/kg). Blood clearance is highest in monkeys (39.0 mL.min-1.kg-1) followed by dogs (38.0 mL.min-1.kg-1) and rats (9.0 mL.min-1.kg-1).
The compound shows marginal to moderate bioactivity in reducing the motility of O. lienalis microfilariae, with a 93.4% reduction, and has been tested for cytotoxicity against Rhesus Monkey LLCMK2 cells. In terms of inhibition of NEK proteins, GSK2008607 exhibits very high inhibition of NEK3 (99.0%) and NEK10 (100.0%), moderate inhibition of NEK4 (49.0%) and NEK5 (24.0%), and lower inhibition of NEK7 (7.1%), NEK9 (6.4%), and NEK11 (1.4%). Minimal inhibition is observed on NEK2 and NEK6 (0.9% each). These results indicate GSK2008607's potential as a targeted inhibitor, particularly against NEK3 and NEK10, as well as its potent anticancer activity through B-Raf V600E mutant inhibition..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | GSK2008607 is a potent B-RafV600E inhibitor with anticancer activity and can be used to study breast, colorectal, melanoma, thyroid, and ovarian cancers. |
| Targets&IC50 | B-Raf:< 0.1 µM, B-Raf:0.008 µM(EC50) |
| Molecular Weight | 667.72 |
| Formula | C31H28F3N7O3S2 |
| Cas No. | 1244644-50-5 |
| Smiles | C(C)(C)C=1SC(=C(N1)C2=C(F)C(NS(=O)(=O)C3=C(F)C=CC=C3F)=CC=C2)C4=NC(NC=5C=CC(=NC5)N6CCOCC6)=NC=C4 |
| Relative Density. | no data available |
| 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: 50 mg/mL (74.88 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
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Calculator
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, and a total of 10 animals are to be administered, using a formulation of 
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 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 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 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.
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
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