GSK215

SKU: orb2900625

Description

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.

Key Properties

• CAS Number: 2743427-26-9
• MW: 985.13
• Purity: >98% (HPLC)
• Formula: C₅₀H₅₉F₃N₁₀O₆S
• SMILES: CNC(=O)c1ccccc1Nc1cc(Nc2ccc(cc2OC)N2CCN(CC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(cc3)-c3scnc3C)C(C)(C)C)CC2)ncc1C(F)(F)F
• Target: FAK
• Solubility: In Vitro: DMSO : 250 mg/mL (253.77 mM; Ultrasonic )

Bioactivity

• In Vivo:
  Animal model: Male CD1 mice (P878/881A), 7-9 weeks. Dosage: 8 mg/kg. Administration: Single subcutaneous injection. Result: Caused a rapid and profound degradation of FAK in liver over time, with a maximal degradation of ~85% being achieved within 18 h. Endogenous FAK was found to still be reduced by ~60% at 96 h post-dose. The Cmax and tmax were 526 ng/mL and 0.33 hours, respectively.
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• In Vitro:
  Western blot analysis. Cell line: A549 cells. Concentration: 0.1-1000 nM Incubation time: 2 h. Result: Increased the FAK degradation. Cell Migration Assay Cell line: A549 cells. Concentration: 100 nM. Incubation time: 48 h. Result: Inhibited cell migration. Cell Invasion Assay Cell line: A549 cells. Concentration: 100 nM. Incubation time: 48 h. Result: Inhibited cell invasion.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

FAK