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FTI-277 hydrochloride

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Catalog No. T2700Cas No. 180977-34-8

Alias FTI 277 HCl

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.

FTI-277 hydrochloride

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Purity: 97.61%

Catalog No. T2700Alias FTI 277 HClCas 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.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	In Stock	In Stock
2 mg	$67	In Stock	In Stock
5 mg	$97	In Stock	In Stock
10 mg	$169	In Stock	In Stock
25 mg	$337	In Stock	In Stock
50 mg	$553	In Stock	In Stock
100 mg	$787	In Stock	In Stock
200 mg	$1,070	-	In Stock
1 mL x 10 mM (in DMSO)	$109	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:97.61%

Color:Transparent

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COA HNMR LCMS

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.
Targets&IC50	FTase:500 pM
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)
Synonyms	FTI 277 HCl

Chemical Properties

Molecular Weight	484.07
Formula	C₂₂H₃₀ClN₃O₃S₂
Cas No.	180977-34-8
Smiles	Cl.Cl.COC(=O)C(CCSC)NC(=O)c1ccc(NCC(N)CS)cc1-c1ccccc1
Relative Density.	no data available

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 12 mg/mL (24.79 mM), Sonication is recommended.

H2O: 14 mg/mL (28.92 mM), Sonication is recommended.

DMSO: 145 mg/mL (299.54 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.82 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/H2O/DMSO

	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

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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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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