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Kobe0065
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。
Kobe0065图片
CAS NO:436133-68-5
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)449.79
FormulaC15H11ClF3N5O4S
CAS No.436133-68-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 89 mg/mL (197.9 mM)
Water: <1 mg/mL
Ethanol: 13 mg/mL (28.9 mM)
Other info
Chemical Name: N-(3-chloro-4-methylphenyl)-2-(2,6-dinitro-4-(trifluoromethyl)phenyl)hydrazinecarbothioamide.
InChi Key: KSJVAYBCXSURMQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C15H11ClF3N5O4S/c1-7-2-3-9(6-10(7)16)20-14(29)22-21-13-11(23(25)26)4-8(15(17,18)19)5-12(13)24(27)28/h2-6,21H,1H3,(H2,20,22,29)
SMILES Code: FC(C1=CC([N+]([O-])=O)=C(NNC(NC2=CC=C(C)C(Cl)=C2)=S)C([N+]([O-])=O)=C1)(F)F
SynonymsKobe-0065; Kobe 0065; Kobe0065
实验参考方法
In Vitro

In vitro activity: Kobe0065-family compounds bind to Ras·GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes. The compounds efficiently inhibit the interaction of Ras·GTP with their multiple effectors including Raf, PI3K, and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases, which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition.


Cell Assay: NIH 3T3 cells are transfected with pEF-BOS-HA-H-Ras(G12V) or an empty vector and treated with the 2 and 20 μM compound or the vehicle (DMSO) in the presence of 2% FBS for 1 h. Cell lysate is subjected to detection of c-Raf-1 coimmunoprecipitated with an anti-H-Ras antibody and total c-Raf-1 by Western blotting with an anti-c-Raf-1 antibody. Immunoprecipitated H-Ras(G12V) are detected by an anti-HA antibody.

In VivoKobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss
Animal modelA xenograft of SW480 cells in nude mice.
Formulation & DosageFormulated in Cremophor:ethanol:water (1:1:6); 80 mg/kg and 160 mg/kg; oral administration
ReferencesProc Natl Acad Sci U S A. 2013 May 14;110(20):8182-7.