CAS NO: | 180977-34-8 |
规格: | ≥98% |
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 |
Molecular Weight (MW) | 484.07 |
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Formula | C22H30ClN3O3S2 |
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 info | Chemical 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 |
Synonyms | FTI-227 HCl; FTI-277; FTI 277; FTI-227 hydrochloride, FTI277; |
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. |
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In Vivo | In mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d i.p.) effectively clears HDV viremia. |
Animal model | HBV/HDV-transgenic FVB mice |
Formulation & Dosage | Dissolved 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. |