SGX-523

Description

A cell-permeable triazolopyridazine compound that acts as a potent, ATP-competitive (Ki = 2.7 & 23 nM using non-phosphorylated and phosphorylated MET kinase domain, respectively), and highly selective inhibitor against the tyrosine kinase activity of the HGF (hepatocyte growth factor) receptor c-MET (IC50 = 4 nM), while exhibiting little or no activity toward a panel of more than 210 other kinases, including the closely related RTK RON. Shown to inhibit the constitutive (IC50 = 40 nM in GTL16 cells) as well as HGF-stimulated (IC50 = 12 nM in A549 cells) MET autophosphorylation/activation in cultures in vitro and effectively suppress MET-dependent tumor growths in mice in vivo (twice daily oral dosings at 30 mg/kg). X-ray crystallography reveals that SGX523 locks MET in a "DFG-in" conformation with the triazolopyridazine moiety interacting with the hydrophobic side chains of Met1229 and Tyr1248, while Tyr1248 mutations are found to render MET insensitive to SGX523 inhibition both in cell-free and cell-based assays.

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

Specification

SGX-523 – FAQ

Q1: Is SGX-523 difficult to dissolve?
A1: SGX-523 dissolves readily in DMSO (2.5 mg/mL), sufficient for most in vitro studies. Guidance is available for higher concentrations and in vivo applications.

Q2: Will batch differences affect reproducibility?
A2: No. Each lot is ≥98% pure and QC-tested to ensure consistent, reliable performance across studies.

Q3: Does resistance from certain MET mutations limit its use?
A3: SGX-523’s defined selectivity makes it an ideal tool for interrogating c-MET signaling and resistance mechanisms in both wild-type and engineered models.

Q4: Is it too costly for in vivo studies?
A4: We offer multiple pack sizes (2–100 mg) for both cell-based assays and large-scale studies—flexible, cost-effective, and with bulk discounts available for larger orders.

Q5: Are there safety concerns when handling SGX-523?
A5: Supplied with full MSDS and handling guidance. Use standard lab PPE; store protected from light at −20 °C.

Q6: Why choose SGX-523 over other MET inhibitors?
A6: SGX-523 is a highly selective, literature-validated c-MET inhibitor with minimal off-target activity—considered a gold-standard tool compound for MET pathway research.

Disclaimer: For laboratory research use only.