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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
FTI-277, when used at 20 micrometers for 48 hours before irradiation, notably decreases the survival of radioresistant HeLa 3A cells expressing a 24-kDa isoform but does not affect the survival of control HeLa PINA cells. This radiosensitizing effect of FTI-277 is accompanied by an increase in postmitotic cell death in HeLa 3A cells and a decrease in G(2)/M phase arrest in both cell lines[1]. GGTI-298 and FTI-277 treatments hinder migration and invasion of PC-3 cells in both time- and dose-dependent manners[3].
体内研究
FTI-277 therapy prevents the rise in PTP-1B and PTEN protein levels seen in burned mice when compared to the vehicle control. Conversely, FTI-277 doesn't significantly change the expression levels of PTP-1B and PTEN in sham-burned mice[2].
体外研究
FTI-277, when used at 20 micrometers for 48 hours before irradiation, notably decreases the survival of radioresistant HeLa 3A cells expressing a 24-kDa isoform but does not affect the survival of control HeLa PINA cells. This radiosensitizing effect of FTI-277 is accompanied by an increase in postmitotic cell death in HeLa 3A cells and a decrease in G(2)/M phase arrest in both cell lines[1].
GGTI-298 and FTI-277 treatments hinder migration and invasion of PC-3 cells in both time- and dose-dependent manners[3].
FTI-277 HCl 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human mesenchymal stem cells (MSC)
5 µM and 10 µM
1 week and 3 weeks
FTI-277 significantly affected osteoblast differentiation (approx. -50±10%) and function (approx. -60±15%), with a higher inhibitory effect at 10 μM. Alendronate reversed the inhibitory effect of FTI-277.
Br J Pharmacol. 2011 Mar;162(5):1109-18.
Human mesenchymal stem cells (MSC)
5 µM and 10 µM
2 weeks
Assessed the effect of FTI-277 on HDJ-2 and prelamin A, finding that FTI-277 inhibited farnesylation of both proteins, with a dose-dependent increase in unfarnesylated protein levels.
Br J Pharmacol. 2011 Mar;162(5):1109-18.
HELN cells
10 µM
24 hours
In HELN cells, FTI-277 and GGTI-298 stimulated basal transcriptional activity by 3.6-fold and 2.4-fold, respectively, in the absence of E2. In the presence of E2, FTI-277 and GGTI-298 further enhanced transcriptional activity by an additional 2.2-fold and 1.6-fold, respectively.
Breast Cancer Res. 2005;7(1):R60-70.
MCF-7 cells
10 µM
24 hours
FTI-277 significantly enhanced E2-induced transcriptional activity. In the absence of E2, FTI-277 and GGTI-298 stimulated basal transcriptional activity by 8.4-fold and 3.9-fold, respectively. In the presence of E2, FTI-277 and GGTI-298 further enhanced transcriptional activity by an additional 4.1-fold and 2.5-fold, respectively.
Breast Cancer Res. 2005;7(1):R60-70.
ESC-derived VEGFR2+ cells
3 µM
4 days
Under low-density culture conditions, FTI-277 significantly reduced PECAM1+ colony numbers and increased αSMA+ colonies, indicating specific inhibition of endothelial differentiation.
J Cell Biol. 2008 Apr 7;181(1):131-41.
MCF7 breast cancer cells
5 µM
48 hours
Combined use of FTI-277 and IPA3 did not significantly inhibit cell proliferation
Mol Cancer. 2013 Aug 6;12(1):88.
A549 lung cancer cells
5 µM
48 hours
Combined use of FTI-277 and IPA3 significantly inhibited cell proliferation
Mol Cancer. 2013 Aug 6;12(1):88.
HT29 colon cancer cells
5 µM
48 hours
Combined use of FTI-277 and IPA3 significantly inhibited cell proliferation
Mol Cancer. 2013 Aug 6;12(1):88.
A375MM melanoma cells
5 µM or 15 µM
48 hours
FTI-277 treatment did not affect PAK protein levels but increased nuclear PhoPAK clusters
Mol Cancer. 2013 Aug 6;12(1):88.
HeLa cells
5 µM or 15 µM
48 hours
After 48 h of FTI-277 treatment, PAK and PhoPAK signals significantly increased
Mol Cancer. 2013 Aug 6;12(1):88.
SH-SY5Y cells
100 nM
48 hours
Reduced the abundance of membrane-associated UCH-L1 (UCH-L1M), decreased α-synuclein levels, and increased cell viability
Proc Natl Acad Sci U S A. 2009 Mar 24;106(12):4635-40.
MCF-7 cells
10 µM
48 hours
To evaluate the effect of FTI-277 on cell proliferation, results showed that FTI-277 treatment significantly inhibited the proliferation of MCF-7 cells.
Cancer Lett. 2010 Jan 28;287(2):172-81.
4T1 cells
10 µM
48 hours
To evaluate the effect of FTI-277 on cell proliferation, results showed that FTI-277 treatment significantly inhibited the proliferation of 4T1 cells.
Cancer Lett. 2010 Jan 28;287(2):172-81.
67NR cells
10 µM
48 hours
To evaluate the effect of FTI-277 on cell proliferation, results showed that FTI-277 treatment significantly inhibited the proliferation of 67NR cells.
Cancer Lett. 2010 Jan 28;287(2):172-81.
ESC-derived VEGFR2+ cells
1 µM
48 hours
FTI-277 added within 3 hours post-VEGF-A stimulation suppressed endothelial differentiation, but no effect when added after 6 hours, demonstrating time-dependent inhibition.
J Cell Biol. 2008 Apr 7;181(1):131-41.
COS-7 cells
100 nM
Decreased the amount of transfected WT UCH-L1M
Proc Natl Acad Sci U S A. 2009 Mar 24;106(12):4635-40.
B16F10 melanoma cells
10 or 20 µM
48 hours
FTI-277 did not enhance membrane FasL expression
Neoplasia. 2007 Dec;9(12):1078-90.
Human bronchial mesenchymal fibroblasts
10 µM
48 hours
To investigate the effect of FTI-277 on TGFβ1-induced fibronectin expression; results showed no significant inhibition of fibronectin accumulation
Respir Res. 2011 Aug 24;12(1):113.
MCF-7 cells
5.9 nM
5 days
To evaluate the inhibitory effects of FTI-277 in combination with different anti-estrogens on MCF-7 cell proliferation. Results showed that FTI-277 combined with Tam had an additive effect, while combinations with ICI182,780 or PBPE exhibited synergistic effects.
Breast Cancer Res. 2005;7(6):R1159-67.
CNE1 cells
1 µM
72 hours
FTI-277 in combination with cisplatin slightly enhanced cytotoxicity in NPC cells with medium CENP-F expression
Mol Cancer. 2010 Sep 9;9:237.
HONE1 cells
1 µM
72 hours
FTI-277 in combination with cisplatin significantly enhanced cytotoxicity in NPC cells with high CENP-F expression
Mol Cancer. 2010 Sep 9;9:237.
Murine bone marrow-derived mast cells
5 µM
72 hours
Inhibition of Ras isoprenylation significantly reduces mast cell degranulation, cytokine production, and migration
2020 Oct 28;11:585070. doi: 10.3389/fimmu.2020.585070.
3T3-L1 cells
20 µM(first 24 h), then 2.5 µM (next 7 days)
8 days
To investigate the effect of FTI-277 on adipogenesis in 3T3-L1 cells. Results showed that FTI-277 increased the number of mature adipocytes, but when combined with non-farnesylated prelamin A accumulation, it reduced the expression of adipogenic genes.
Int J Mol Sci. 2024 Jan 20;25(2):1282.
CHO-K1 cells
1 µM
8 hours
An 8 h treatment with 1μM FTI-277 led to an increase in p27 expression in cells that were selected before analysis for H-2Kk expression on magnetic beads conjugated to a monoclonal antibody against H-2Kk.
EMBO Rep. 2004 Jul;5(7):721-7.
HeLa cells
1 µM
8 hours
Addition of FTI-277 resulted in a 10- to 20-fold increase in LucF translation with a reporter containing the R17-binding site.
EMBO Rep. 2004 Jul;5(7):721-7.
SK-Hep1 cells
1 µM
8 hours
FTI-277 prevents the membrane association of the CAAX motif and thus increases the cytoplasmic levels of the eIF4G fusion protein, which is then capable of inducing translation of the second cistron of a bicistronic messenger RNA containing an R17-binding site in its intercistronic space.
EMBO Rep. 2004 Jul;5(7):721-7.
FTI-277 HCl 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
E6.75 whole-embryo culture model
In vitro culture medium
10 μM
Single dose, cultured for 3 days
FTI-277 treatment diminished PECAM1+ vessels in yolk sacs, with decreased PECAM1 and VE-cadherin mRNA levels but unchanged αSMA expression, suggesting suppression of vascular development.
J Cell Biol. 2008 Apr 7;181(1):131-41.
Mice
Dopaminergic neurons in midbrain mixed primary cultures
Added to culture medium
100 nM
Single treatment, duration not specified
Reduced α-synuclein toxicity
Proc Natl Acad Sci U S A. 2009 Mar 24;106(12):4635-40.
Mice
HBV transgenic mice
Intraperitoneal injection
50 mg/kg/day
Once daily for 7 days
FTI-277 and FTI-2153 were both highly effective at clearing HDV viremia
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