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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $127 | In Stock | |
5 mg | $317 | In Stock | |
10 mg | $497 | In Stock | |
25 mg | $829 | In Stock | |
50 mg | $1,150 | In Stock | |
100 mg | $1,550 | In Stock |
Description | GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4). GSK215 is designed by the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase. GSK215 can induce 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]. |
Molecular Weight | 985.13 |
Formula | C50H59F3N10O6S |
Cas No. | 2743427-26-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 225.0 mg/mL (228.4 mM ) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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