GSK215
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. 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].
Product Specifications
CAS Number
2743427-26-9
UNSPSC
12352005
Hazard Statement
H315, H319, H320
Target
FAK; PROTACs
Type
Reference compound
Related Pathways
PROTAC; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/gsk215.html
Purity
99.26
Solubility
DMSO : 250 mg/mL (ultrasonic)
Smiles
O=C([C@H]1N(C([C@@H](NC(CN2CCN(C3=CC=C(NC4=NC=C(C(F)(F)F)C(NC5=CC=CC=C5C(NC)=O)=C4)C(OC)=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
Molecular Formula
C50H59F3N10O6S
Molecular Weight
985.13
Precautions
H315, H319, H320
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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