SBI-0206965
SBI-0206965 Basic information
- Product Name:
- SBI-0206965
- Synonyms:
-
- SBI-0206965
- SBI0206965; SBI-0206965; SBI 0206965.
- CS-1581
- SBI 0206965;SBI0206965
- 2-((5-Bromo-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)oxy)-N-methylbenzamide
- SBI-0206965（02）
- Benzamide, 2-[[5-bromo-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]oxy]-N-methyl-
- SBI-0206965,SBI 0206965,inhibit,Inhibitor,Unc-51 like kinase,Apoptosis,Autophagy,ULK
- CAS:
- 1884220-36-3
- MF:
- C21H21BrN4O5
- MW:
- 489.32
- Product Categories:
-
- Inhibitors
- Mol File:
- 1884220-36-3.mol
SBI-0206965 Chemical Properties
- Melting point:
- 170 - 172°C
- Density
- 1.434±0.06 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- Soluble in DMSO (up to 30 mg/ml)
- form
- powder
- pka
- 14.80±0.46(Predicted)
- color
- white to beige
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
SBI-0206965 Usage And Synthesis
Description
ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM). It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells. SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 . It also blocks ULK1-dependent cell survival following nutrient deprivation.
Uses
SBI-0206965 is an inhibitor of ULK1. It also blocks ULK1-dependent cell survival following nutrient deprivation. ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation.
Biochem/physiol Actions
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.
in vivo
SBI-0206965 (50?mg/kg; i.p.; once every 3 days for 37 days) inhibites tumour growth and induces apoptosis in A498 xenograft tumours[1].
| Animal Model: | Six-week-old male BALB/c nude mice (A498 xenograft tumours)[1] |
| Dosage: | 50?mg/kg |
| Administration: | Intraperitoneal injection; once every three days for 37 days |
| Result: | Significantly suppressed tumour growth. |
IC 50
ULK1: 108 nM (IC50); ULK2: 711 nM (IC50)
References
[1] DANIEL F EGAN. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates.[J]. Molecular Cell, 2015: 285-297. DOI:10.1016/j.molcel.2015.05.031
SBI-0206965Supplier
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