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FTI-277 hydrochloride

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Purity:98.19%

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COA HNMR HPLC

FTI-277 hydrochloride

Catalog No. T2700Cas No. 180977-34-8

FTI-277 hydrochloride (FTI 277 HCl) is an effective and specific farnesyltransferase (FTase) inhibitor (IC50: 500 pM); this selectivity is about 100-fold than the closely related GGTase I.

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Pack Size	Price	Availability
1 mg	$48	In Stock
2 mg	$67	In Stock
5 mg	$97	In Stock
10 mg	$185	In Stock
25 mg	$337	In Stock
50 mg	$565	In Stock
100 mg	$793	In Stock
1 mL x 10 mM (in DMSO)	$113	In Stock

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Product Introduction

Bioactivity

Description	FTI-277 hydrochloride (FTI 277 HCl) is an effective and specific farnesyltransferase (FTase) inhibitor (IC50: 500 pM); this selectivity is about 100-fold than the closely related GGTase I.
In vitro	In mouse models infected with Hepatitis B Virus (HBV) and Hepatitis D Virus (HDV), FTI-277 administered intraperitoneally at a dosage of 50 mg/kg/day effectively clears Hepatitis D viremia.
In vivo	In drug-resistant myeloma cells, FTI-277 inhibits cell growth and induces apoptosis. It mitigates the toxicity induced by methamphetamine in SH-SY5Y cells through effects on cell degeneration, activation, the c-Jun N-terminal kinase cascade, and the Ras activation process. FTI-277 inhibits Ras processing (IC50: 100 nM) without affecting the overall cellular prenylation of Rap1A. Additionally, FTI-277 increases post-irradiation apoptosis and enhances the radiation sensitivity of H-ras transformed rat embryo cells.
Kinase Assay	FTase and GGTase I Activity 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 Research	Cells 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. (Only for Reference)
Alias	FTI 277 HCl

Chemical Properties

Molecular Weight	484.07
Formula	C22H30ClN3O3S2
Cas No.	180977-34-8

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 12 mg/mL (24.8 mM)

H2O: 14 mg/mL (28.9 mM)

DMSO: 89 mg/mL (183.9 mM)

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.0658 mL	10.3291 mL	20.6582 mL	103.2908 mL
5 mM	0.4132 mL	2.0658 mL	4.1316 mL	20.6582 mL
10 mM	0.2066 mL	1.0329 mL	2.0658 mL	10.3291 mL
20 mM	0.1033 mL	0.5165 mL	1.0329 mL	5.1645 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0413 mL	0.2066 mL	0.4132 mL	2.0658 mL
100 mM	0.0207 mL	0.1033 mL	0.2066 mL	1.0329 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

You can also refer to dose conversion for different animals. More

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc