GSK215

Product Name: GSK215
CAS No.: 2743427-26-9
Chemical 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
CBNumber: CB810705803
Molecular Formula: C50H59F3N10O6S
Formula Weight: 985.14
MOL File: 2743427-26-9.mol

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GSK215 Property

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

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Hazard and Precautionary Statements (GHS)

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GSK215 Chemical Properties,Usage,Production

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

Raw materials

Preparation Products

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GSK215 Suppliers

China 38 United States 2 Global 40

Changzhou Borl Biotechnology Co.,LTD

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View Lastest Price from GSK215 manufacturers

Hubei Chuchang Biotech Co., Ltd.

Product: GSK215 2743427-26-9
Price: US $0.00-0.00/mg
Min. Order: 1mg
Purity: 98%
Supply Ability: 100G
Release date: 2024-04-17

2743427-26-9, GSK215Related Search:

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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

2743427-26-9

C50H59F3N10O6S