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关于此项目
经验公式(希尔记法):
C18H17N5O3
化学文摘社编号:
分子量:
351.36
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
DMSO: 0.5 mg/mL
shipped in
wet ice
storage temp.
−20°C
SMILES string
[n]21[c](c3c(nc2NC(=O)c4cnccc4)c(c(cc3)OC)OC)=NCC1
InChI
1S/C18H17N5O3/c1-25-13-6-5-12-14(15(13)26-2)21-18(23-9-8-20-16(12)23)22-17(24)11-4-3-7-19-10-11/h3-7,10H,8-9H2,1-2H3,(H,21,22,24)
InChI key
ZJAVHOMVDCMAMF-UHFFFAOYSA-N
General description
一种具有细胞渗透性的咪唑喹唑啉化合物,可作为一种针对全部三类PI 3-K激酶(p110α,p110γ、PI 3-KC2α,p110δ,PI 3-KC2β,p110β和hsVPS34的IC50 分别为11,18、47、58、64、350和830 nM)以及几种PIKK(DNA-PK,ATM和mTORC1的IC50 分别为13、610和1050 nM)和PI 4-KIIIα(IC50 =830 nM)的强效、可逆的ATP竞争性抑制剂,同时对PI 4-KIIIβ和ATR的效价大大降低(分别为IC50 =3.1和15 µM),对PI 4-KIIα,PIPK(IC50 >100 µM)以及一组36种常用研究的蛋白激酶(在2.5 µM时为<15% inhibition at 10 µM). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90%)的活性很小或没有活性,并完全防止小鼠体内胰岛素诱导的血糖下降(10 mg/ml,i.p.)。
Packaging
用惰性气体包装
Preparation Note
复溶后,等分并冷冻保存(-20°C)。贮备液在-20°C下可稳定保存至多3个月。
完全溶解可能需要轻微加热。
Other Notes
Fan, Q.W., et al. 2007.Cancer Res.67, 7960.
Fan, Q.W., et al. 2006.Cancer Cell9, 341.
Knight, Z.A., et al. 2006.Cell125, 733.
Fan, Q.W., et al. 2006.Cancer Cell9, 341.
Knight, Z.A., et al. 2006.Cell125, 733.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性:标准处理(A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable