SML1540

SBI-0206965

≥98% (HPLC), serine/threonine autophagy-initiating kinases ULK1 and ULK2 inhibitor, powder

• Sinónimos: 2-((5-Bromo-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)oxy)-N-methylbenzamide
• Fórmula empírica (notación de Hill): C₂₁H₂₁BrN₄O₅
• Número CAS: 1884220-36-3
• Peso molecular: 489.32
• UNSPSC Code: 12352200
• PubChem Substance ID: 329825951
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Propiedades

• Nombre del producto: SBI-0206965, ≥98% (HPLC)
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 20 mg/mL, clear
• storage temp.: −20°C
• SMILES string: 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)
• InChI key: NEXGBSJERNQRSV-UHFFFAOYSA-N

Descripción

Application

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

Biochem/physiol Actions

SBI-0206965 is a potent and selective inhibitor of the serine/threonine autophagy-initiating kinases ULK1 and ULK2 with selectivity for ULK1.

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.

Información de seguridad

• Pictogramas: GHS07
• Palabra de advertencia: Warning
• Códigos de peligro: H315,H319,H335
• Indicaciones de precaución: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Hazard Classifications: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Órganos diana: Respiratory system
• Clase de almacenamiento: 11 - Combustible Solids
• ¿Qué está pasando?: WGK 3
• Punto de inflamación (°F): Not applicable
• Punto de inflamación (°C): Not applicable