SML1540

SBI-0206965

≥98% (HPLC)

• Synonyme(s) : 2-((5-Bromo-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)oxy)-N-methylbenzamide
• Formule empirique (notation de Hill): C₂₁H₂₁BrN₄O₅
• Numéro CAS: 1884220-36-3
• Poids moléculaire : 489.32
• Code UNSPSC : 12352200
• ID de substance PubChem : 329825951
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 20 mg/mL, clear
• Température de stockage: −20°C
• Chaîne SMILES: BrC1=C(OC2=C(C(NC)=O)C=CC=C2)N=C(NC3=CC(OC)=C(OC)C(OC)=C3)N=C1
• InChI: 1S/C21H21BrN4O5/c1-23-19(27)13-7-5-6-8-15(13)31-20-14(22)11-24-21(26-20)25-12-9-16(28-2)18(30-4)17(10-12)29-3/h5-11H,1-4H3,(H,23,27)(H,24,25,26)
• Clé InChI: NEXGBSJERNQRSV-UHFFFAOYSA-N

Description

Application

SBI-0206965 has been used to study its effect on the growth of cadmium-transformed prostate epithelial cells.

Actions biochimiques/physiologiques

SBI-0206965 is a potent and selective inhibitor of the serine/threonine autophagy-initiating kinases ULK1 and ULK2 with selectivity for ULK1. SBI-0206965 has an IC₅₀ value of 108 nM for ULK1, compared to 711nM for ULK2. Tumor cells require autophagy to remove misfolded proteins or damaged cellular organelles. SBI-0206965 was shown to suppress autophagy induced by mTOR inhibition. mTOR signaling is often hyperactive in many tumors and can drive proliferation, so mTOR inhibitors are being investigated as anticancer agents. However, mTOR inhibition also results in activation of the ULK1-dependent autophagy survival response, and most results with mTOR inhibitors have been at best cytostatic. SBI-0206965 synergizes with mTOR inhibition to induce apoptosis and cell death.

Since most of the tumor cells survive on autophagy mechanism, inhibition of autophagy inducers Unc-51 (serine/threonine-protein kinase)-like autophagy activating kinase (ULK1 and ULK2) might be useful in cancer therapy.

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H315,H319,H335
• Conseils de prudence: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Classification des risques: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Organes cibles: Respiratory system
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable