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SBI-0206965
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SBI-0206965图片
CAS NO:1884220-36-3
规格:≥98%
包装与价格:
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

产品介绍
理化性质和储存条件
Molecular Weight (MW)489.32
FormulaC21H21BrN4O5
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.

实验参考方法
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 VivoSBI-0206965 (50 mg/kg; i.p.; once every 3 days for 37 days) inhibites tumour growth and induces apoptosis in A498 xenograft tumors
Animal modelA498 xenograft tumor
Formulation & Dosage50 mg/kg; i.p.
References

Mol Cell. 2015 Jul 16;59(2):285-97; EBioMedicine. 2018 Aug;34:85-93.