1. Protein Tyrosine Kinase/RTK
    PROTAC
  2. FAK
    PROTAC
  3. GSK215

GSK215 

Cat. No.: HY-132296
Handling Instructions

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.

For research use only. We do not sell to patients.

GSK215 Chemical Structure

GSK215 Chemical Structure

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Description

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].

IC50 & Target

PROTAC; DC50: 1.3 nM (FAK)

In Vitro

GSK215 (0.1-1000 nM; 2 hours) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0.1-1000 nM
Incubation Time: 2 hours
Result: Increased the FAK degradation.
In Vivo

GSK215 (8mg/kg; i.h.) treatment shows the Cmax and tmax values of 526 ng/mL and 0.33 hours, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD1 mice (P878/881A)[1]
Dosage: 8 mg/kg
Administration: I.u.(Pharmacokinetic Analysis)
Result: The Cmax and tmax were 526 ng/mL and 0.33 hours, respectively.
Molecular Weight

985.13

Formula

C₅₀H₅₉F₃N₁₀O₆S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Product Name:
GSK215
Cat. No.:
HY-132296
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