FTI-2153 TFA

Name: FTI-2153 TFA
Brand: MedChemExpress
SKU: HY-123242A
Rating: 4.5 (1 reviews)

Cat. No.: HY-123242A Purity: 99.11%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

FTI-2153 TFA is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC₅₀ of 1.4 nM. FTI-2153 TFA is >3000-fold more potent at blocking H-Ras (IC₅₀, 10 nM) than Rap1A processing. Anti-cancer activity.

For research use only. We do not sell to patients.

FTI-2153 TFA Chemical Structure

CAS No. : 2820151-01-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 575	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 575	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1550	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2350	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3400	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

In Vitro

FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status in two human lung cancer cell lines^[2].
FTI-2153 increases the percentage of prometaphase cells with ring-like DNA morphology in transformed and non-transformed cells^[2].
FTI-2153 (15 μM) inhibits T-24 and Calu-1 cell growth by 38 and 36%, respectively. NIH3T3, HFF and HT-1080 are less sensitive and are inhibited by only 8, 8 and 13%, respectively. A-549 and OVCAR3 cell growth is inhibited by 25 and 22%, respectively. Thus, even though T-24 and Calu-1 cells are equisensitive to FTI-2153 cell growth inhibition, FTI-2153 inhibits bipolar spindle formation only in Calu-1 cells. HFF and NIH3T3 cells are both resistant to FTI2153 growth inhibition, yet only NIH3T3 cells are resistant to FTI-2153 inhibition of bipolar spindle formation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:	NIH3T3, HFF, HT1080, T-24, OVCAR3, A-549 and Calu-1 CELLS.
Concentration:	48 h.
Incubation Time:	15 μM.
Result:	When A-549 cells were treated with FTI-2153 (15 μM for 48 h), the proportion of cells at prometaphase increased relative to the other phases of mitosis. FTI-2153 accumulated cells at prometaphase with a rosette-like morphology where chromosomes form a ring surrounding a monoaster of microtubules. In all cells, except for T-24 and NIH3T3, FTI-2153 treatment increased the proportion of mitotic cells in prometaphase and decreased the percentage of cells in telophase/cytokinesis. In HT1080 cells, the percentage of cells in prometaphase and telophase/ cytokinesis were 5 and 85% in control cells and 55 and 35% in Treated cells, respectively. Similarly results were also found in HFF cells. Calu-1 and A-549 cells, as described previously, had similarly large changes, whereas OVCAR3 had smaller changes. In contrast, FTI-2153 did not significantly affect the distribution of the different phases of mitosis in T-24 and NIH3T3 cells.

Molecular Weight

580.62

Formula

C₂₇H₃₁F₃N₄O₅S

CAS No.

2820151-01-5

Appearance

Solid

Color

White to off-white

SMILES

CSCC[C@@H](C(OC)=O)NC(C1=CC=C(CNCC2=CN=CN2)C=C1C3=CC=CC=C3C)=O.OC(C(F)(F)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 90 mg/mL (155.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7223 mL	8.6115 mL	17.2230 mL
5 mM	0.3445 mL	1.7223 mL	3.4446 mL
10 mM	0.1722 mL	0.8611 mL	1.7223 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.25 mg/mL (3.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.25 mg/mL (3.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.25 mg/mL (3.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.11%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (251 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[1]. Sun J, et al. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine. Cancer Res. 1999 Oct 1;59(19):4919-26. [Content Brief]

[2]. N C Crespo, et al. The farnesyltransferase inhibitor, FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status. Cell Death Differ. 2002 Jul;9(7):702-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7223 mL	8.6115 mL	17.2230 mL	43.0574 mL
	5 mM	0.3445 mL	1.7223 mL	3.4446 mL	8.6115 mL
	10 mM	0.1722 mL	0.8611 mL	1.7223 mL	4.3057 mL
	15 mM	0.1148 mL	0.5741 mL	1.1482 mL	2.8705 mL
	20 mM	0.0861 mL	0.4306 mL	0.8611 mL	2.1529 mL
	25 mM	0.0689 mL	0.3445 mL	0.6889 mL	1.7223 mL
	30 mM	0.0574 mL	0.2870 mL	0.5741 mL	1.4352 mL
	40 mM	0.0431 mL	0.2153 mL	0.4306 mL	1.0764 mL
	50 mM	0.0344 mL	0.1722 mL	0.3445 mL	0.8611 mL
	60 mM	0.0287 mL	0.1435 mL	0.2870 mL	0.7176 mL
	80 mM	0.0215 mL	0.1076 mL	0.2153 mL	0.5382 mL
	100 mM	0.0172 mL	0.0861 mL	0.1722 mL	0.4306 mL

FTI-2153 TFA Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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FTI-2153 TFA

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