GSK215 - ≥99% , CAS No.2743427-26-9

CAS: 2743427-26-9 Cat. No.: G648707 Summenformel: C₅₀H₅₉F₃N₁₀O₆S Molekulargewicht: 985.13

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Application

PROTAC

Übersicht

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a p DC 50 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

In Vitro

GSK215 (0.1-1000 nM; 2 h) effectively increases the FAK degradation by >90% and determines a DC 50 of 1.3 nM in A549 cells. GSK215 induced degradation is proteasome and ubiquitin dependent. GSK215 (above 100 nM, 6h) reduces primarily kinases CDK7, RPS6KA3, MET and GAK. GSK215 (100 nM, 48 h) inhibits migration, invasion and collagen deposition in A549 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: A549 cells Concentration: 0.1-1000 nM Incubation Time: 2 h Result: Increased the FAK degradation. Cell Migration AssayCell Line: A549 cells Concentration: 100 nM Incubation Time: 48 h Result: Inhibited cell migration. Cell Invasion AssayCell Line: A549 cells Concentration: 100 nM Incubation Time: 48 h Result: Inhibited cell invasion.

In Vivo

GSK215 (8 mg/kg; i.h.; once) degrades FAK, and shows the C max and t max values of 526 ng/mL and 0.33 hours, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 C max and t max were 526 ng/mL and 0.33 hours, respectively.

Form:Solid

IC50& Target:PROTAC,pDC 50 : 8.4 (FAK)

Specifications

Spezifikationen & Reinheit

≥99%

Biochemische und physiologische Mechanismen

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a p DC 50 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-lasti

Storage

Store at -20°C

Verschickt in

Ice chest + Ice pads

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

INHIBITOR

Reinheit

≥99%

Namen und Kennungen

Molekulargewicht

985.13

Chemische und physikalische Eigenschaften

• Löslichkeit: DMSO : 250 mg/mL (253.77 mM; Need ultrasonic)

Häufig gestellte Fragen

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2743427-26-9, the molecular formula is C50H59F3N10O6S, and the molecular weight is 985.13 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.