SGX-523

SKU: orb1305777

Description

SGX-523

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1022150-57-7
• MW: 359.41
• Purity: 99.49%
• Formula: C₁₈H₁₃N₇S
• SMILES: Cn1cc(cn1)-c1ccc2nnc(Sc3ccc4ncccc4c3)n2n1
• Target: p38 MAPK,Bcr-Abl,c-Met/HGFR,Raf
• Solubility: DMSO:3.6 mg/mL (10.02 mM)

Bioactivity

• Target IC50:
  MET:4 nM
• In Vivo:
  SGX523, at nanomolar concentration , inhibits MET-regulated signaling, cell proliferation, and migration without affecting signals dependent on Other protein kinases, such as RON, even at micromolar levels. In vivo SGX523 dose-dependently inhibit the growth of xenografts derived from human malignant gliomas, lung cancer, and gastric cancer, indicating these tumors' reliance on MET's catalytic activity. SGX-523 acts as a c-Met/hepatocyte growth factor receptor tyrosine kinase inhibitor, deactivating MET and preventing its interaction with Other protein kinases. It significantly inhibit the catalytic domain of purified MET while having no effect on closely related RON. As an ATP-competitive inhibitor, SGX523 shows a higher affinity for low-activity and non-phosphorylated MET (MET-KD(0P), Ki: 2.7 nM).
• In Vitro:
  SGX523, administered orally twice daily at a dose of ≥10 mg/kg, significantly delay the anticipated growth of GTL16 tumors. At a higher concentration of 30 mg/kg, SGX523 not only markedly inhibit the growth of U87 mg tumors but also delay the growth of H441 tumors, while reducin the levels of MET autophosphorylation.
• Cell Research:
  MDCK cells are seeded at 1 × 103 per well in a 24-well plate and incubated at 37℃n 5% CO2 for 1 week in MEM and 10% fetal bovine serum. HGF (90 ng/mL) and various concentration of SGX523 are added an the cells are incubated for a Other 18 hours (37℃, 5% CO2 humidified incubator) and visualized. A549 cells are plated in 12-well plates (6 × 10^4 per well) and incubated to confluence to investigate cell migration. A channel is introduced int the monolayers by scratching with a pipette tip. Various dilutions of compound are added in starve medium in the presence and absence of HGF (90 ng/mL).The wells are checked for cell migration after twenty-fou(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

c-Met, cMet, c-Met/HGFR, cMet/HGFR, C-Raf, antitumor, B-Raf (V599E), BcrAbl, Abl, inhibit, Inhibitor, MET, HGFR, exquisitely, SGX 523, SGX523, SGX-523, p38α, p38MAPK, selective, p38 MAPK

Compound Identifiers

PubChem CID

24779724