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FTI 277 HCl
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。
FTI 277 HCl图片
CAS NO:180977-34-8
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
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)484.07
FormulaC22H30ClN3O3S2
CAS No.180977-34-8(HCl);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 96 mg/mL (198.3 mM)
Water: 17 mg/mL (35.1 mM)
Ethanol: 14 mg/mL (28.9 mM)
Other infoChemical Name: methyl (5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-carbonyl)-L-methioninate hydrochloride
InChi Key: PIAFFJUUNXEDEW-PXPMWPIZSA-N
InChi Code: InChI=1S/C22H29N3O3S2.ClH/c1-28-22(27)20(10-11-30-2)25-21(26)18-9-8-17(24-13-16(23)14-29)12-19(18)15-6-4-3-5-7-15;/h3-9,12,16,20,24,29H,10-11,13-14,23H2,1-2H3,(H,25,26);1H/t16-,20+;/m1./s1
SMILES Code: CSCC[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2)=O.[H]Cl
SynonymsFTI-227 HCl; FTI-277; FTI 277; FTI-227 hydrochloride, FTI277;
实验参考方法
In Vitro

In vitro activity: FTI-277 inhibits Ras processing with an IC50 of 100 nM, but not the geranylgeranylated Rap1A processing in whole cells. FTI-277 induces accumulation of cytoplasmic non-farnesylated H-Ras, accumulates inactive Ras/Raf complexes in the cytoplasm, and blocks constitutive MAPK activation in H-RasF cells. FTI-277 causes increased apoptosis after irradiation and increases radiosensitivity in H-ras-transformed rat embryo cells. FTI-277 also inhibits cell growth and induces apoptosis in drug-resistant myeloma tumor cells. In SH-SY5Y cells, FTI-277 diminishes the toxic effects of methamphetamine on induction in cell degeneration, activation in c-Jun-N-terminal kinase cascades, and Ras activation.


Kinase Assay: FTase and GGTase I activities from 60,000×g supernatants of human Burkitt lymphoma (Daudi) cells are assayed. Inhibition studies are performed by determining the ability of Ras CAAX peptidomimetics to inhibit the transfer of [3H]farnesyl and [3H]geranylgeranyl from [3H]farnesylpyrophosphate and [3H]geranylgeranylpyrophosphate to H-Ras-CVLS and H-Ras-CVLL, respectively.


Cell Assay: Cells (8226, U266, and H929 multiple myeloma cell lines) are seeded at 8000–14 000 cells/well in 96-well plates. To establish a dose–response to FTI-277, cells are incubated for 96 h in two-fold serial dilutions ranging from 3.75 times 10-7 M to 1 times 10-5 M. Following continuous drug exposure, 50 μL MTT dye is added. The insoluble formazan complex is solubilized with DMSO and absorbance measured at 540 nm. IC50s and 95% confidence intervals are calculated by regression analysis of the linear portion of the dose–response curve.

In VivoIn mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d i.p.) effectively clears HDV viremia.
Animal modelHBV/HDV-transgenic FVB mice
Formulation & DosageDissolved in 5% DMSO, 0.5 mM DTT in sterile saline; 50 mg/kg; i.p. injection
References

J Biol Chem. 1995 Nov 10;270(45):26802-6; Cancer Res. 1996 Apr 15;56(8):1727-30; J Clin Invest. 2003 Aug;112(3):407-14.