| CAS NO: | 1884220-36-3 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 489.32 |
|---|---|
| Formula | C21H21BrN4O5 |
| CAS No. | 1884220-36-3 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 97 mg/mL (198.2 mM) |
| Water: < 1 mg/mL | |
| Ethanol: 10 mg/mL (20.4 mM) | |
| Other info | Chemical Name: 2-((5-bromo-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)oxy)-N-methylbenzamide InChi Key: NEXGBSJERNQRSV-UHFFFAOYSA-N InChi Code: 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) SMILES Code: O=C(NC)C1=CC=CC=C1OC2=NC(NC3=CC(OC)=C(OC)C(OC)=C3)=NC=C2Br |
| Synonyms | SBI0206965; SBI-0206965; SBI 0206965. |
| In Vitro | In vitro activity: In HEK293T transfected with WT or KI Myc-tagged ULK1 and WT Vps34, SBI-0206965 inhibits Ser249 phosphorylation of overexpressed Vps34 and Beclin1 Ser15 phosphorylation. SBI-0206965 suppresses autophagy induced by mTOR inhibition in A549 cells, and prevents ULK1-dependent cell survival in WT MEFs. In addition, SBI-0206965 also synergizes with mTOR inhibition to induce cancer cell death. Cell Assay: In HEK293T cells transfected with WT or KI Myc-tagged ULK1 and WT Vps34, SBI-0206965 inhibited Ser249 phosphorylation of overexpressed Vps34 at the dose of ~ 5 μM. In HEK293T cells, it was found that SBI-0206965 also inhibited the phosphorylation of Beclin1 Ser15 to comparable extents. |
|---|---|
| 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 tumors |
| Animal model | A498 xenograft tumor |
| Formulation & Dosage | 50 mg/kg; i.p. |
| References | Mol Cell. 2015 Jul 16;59(2):285-97; EBioMedicine. 2018 Aug;34:85-93. |
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