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RBC8
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。
RBC8图片
CAS NO:361185-42-4
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

产品介绍
理化性质和储存条件
Molecular Weight (MW)424.45
Formula C25H20N4O3
CAS No. 361185-42-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 40 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo) N#CC(C1C2=CC(OC)=CC=C2OC)=C(N)OC3=C1C(C4=CC=C5C=CC=CC5=C4)=NN3
Synonyms RBC8; RBC-8; RBC 8.
实验参考方法
In Vitro

In vitro activity: In living cells, RBC8 also reduces the activation of RalA by inducing chemical shift changes in RalB–GDP. In Ral-dependent lines H2122 and H358, RBC8 causes anchorage-independent growth inhibition with IC50 of 3.5 μM and 3.4 μM, respectively


Kinase Assay:His-RalA (100 ng) was incubated with gamma-labeled 32P-GTP (8 nM assay concentration) and either DMSO or individual compounds (50 μM assay concentration) dissolved in DMSO in the presence of EDTA (20 mM) for 15 min at 30°C. The reaction was stopped by dilution into excess MgCl2, and the incorporation of radiolabeled nucleotide was measured by filter binding. 32P-GTP (alpha-labeled) was converted to 32P-GDP by nucleotide diphosphokinase, and used for the binding assay with GDP.


Cell Assay: Growth inhibition of human lung cancer cells by the compounds is measured under anchorage-independent conditions in soft agar. Cells are seeded into 6-well plates (coated with a base layer made of 2.0 ml of 1% low-melting-point agarose) at 15,000 cells per well in 3.0 mL of 0.4% low-melting-point agarose containing various concentration of drug. Two to four weeks (depending on the cell line) after incubation, the cells are stained with 1.0 mg ml–1 nitroblue tetrazolium, and colonies are counted under a microscope. The IC50 values are defined as the concentration of drug that resulted in a 50% reduction in colony number compared with the DMSO-treated control.

In Vivo In mice bearing H358 xenografts, RBC8 (50 mg/kg i.p.) inhibits tumor growth via specific inhibition of RalA and RalB
Animal model Mice bearing H358 xenografts
Formulation & Dosage DMSO,50 mg/kg, i.p.
References Nature. 2014 Nov 20;515(7527):443-7.