GSK215 manufacturers
- GSK215
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- $0.00 / 10mg
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2024-07-22
- CAS:2743427-26-9
- Min. Order: 1mg
- Purity: 98%
- Supply Ability: 100G
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| Product Name: | GSK215 | | Synonyms: | GSK215;(2S,4R)-4-hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-((4-((2-(methylcarbamoyl)phenyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide | | CAS: | 2743427-26-9 | | MF: | C50H59F3N10O6S | | MW: | 985.14 | | EINECS: | | | Product Categories: | | | Mol File: | 2743427-26-9.mol |  |
| | GSK215 Chemical Properties |
| Boiling point | 1103.2±65.0 °C(Predicted) | | density | 1.317±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 250 mg/mL (253.77 mM; Need ultrasonic) | | form | Solid | | pka | 13.97±0.40(Predicted) | | color | Off-white to light yellow | | InChIKey | ZGSWGXNEXAXEGV-VSAGVCMVNA-N |
| | GSK215 Usage And Synthesis |
| Biological Activity | GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect[1].
GSK215 (0.1-1000 nM; 2 hours) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM[1].
GSK215 (8mg/kg; i.h.) treatment shows the Cmax and tmax values of 526 ng/mL and 0.33 hours, respectively[1]. | | in vitro | 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. Its induced degradation is proteasome and ubiquitin-dependent. GSK215 (above 100 nM, 6h) primarily reduces kinases CDK7, RPS6KA3, MET, and GAK. This compound (100 nM, 48 h) inhibits migration, invasion, and collagen deposition in A549 cells.
| | storage | Store at -20°C | | References | [1]. Law RP, Nunes J, Chung CW, et al. Discovery and Characterisation of Highly Cooperative FAK-Degrading PROTACs [published online ahead of print, 2021 Aug 20]. Angew Chem Int Ed Engl. 2021;10.1002/anie.202109237. |
| | GSK215 Preparation Products And Raw materials |
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