FGTI-2734 mesylate

Name: FGTI-2734 mesylate
Brand: MedChemExpress
SKU: HY-128350A
Rating: 4.5 (1 reviews)

Cat. No.: HY-128350A Purity: 99.65%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC₅₀s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.

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

FGTI-2734 mesylate Chemical Structure

CAS No. : 2702297-24-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 200	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 200	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 810	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1300	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of FGTI-2734 mesylate:

FGTI-2734 Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 250 nM (FT) and 520 nM (GGT)^[1]

In Vitro

FGTI-2734 mesylate (1-30 μM; 72 hours) induces apoptosis in mutant KRAS-dependent, but not mutant KRAS- independent, human cancer cells^[1].
FGTI-2734 mesylate (3-30 μM; 72 hours) inhibits both protein prenylation of HDJ2, RAP1A, KRAS and NRAS. FGTI-2734 inhibits KRAS membrane localization in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells^[1].

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

Apoptosis Analysis^[1]

Cell Line:	MiaPaCa2, L3.6pl, Calu6 cells
Concentration:	1, 3, 10, 30 μM
Incubation Time:	72 hours
Result:	Induced apoptosis in mutant KRAS-dependent human cancer cell lines

Western Blot Analysis^[1]

Cell Line:	KRAS, HRAS, and NRAS-transformed NIH3T3 cells
Concentration:	3, 10, 30 μM
Incubation Time:	72 hours
Result:	Inhibited both protein prenylation of HDJ2, RAP1A, KRAS and NRAS.

In Vivo

FGTI-2734 mesylate (intraperitoneally; 100 mg/kg/day for 18 to 25 days) only inhibits tumor growth in mutant KRAS-dependent tumors but not in mutant KRAS-independent tumors^[1].

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

Animal Model:	Male SCID-bg mice following injection of MiaPaCa2, L3.6pl, Calu6, A549, H460 and DLD1 cancer cells^[1]
Dosage:	100 mg/kg
Administration:	Intraperitoneally; daily; for 18 to 25 days
Result:	Inhibited tumor growth in mutant KRAS-dependent tumors.

Molecular Weight

606.73

Formula

C₂₇H₃₅FN₆O₅S₂

CAS No.

2702297-24-1

Appearance

Solid

Color

White to off-white

SMILES

OS(=O)(C)=O.O=S(C1=NC=CC=C1)(N(CCN(C2=CC=C(C#N)C=C2F)CC3=CN=CN3C)CC4CCCCC4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 75 mg/mL (123.61 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	1.6482 mL	8.2409 mL	16.4818 mL
5 mM	0.3296 mL	1.6482 mL	3.2964 mL
10 mM	0.1648 mL	0.8241 mL	1.6482 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 (sealed storage, away from moisture). 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: ≥ 3 mg/mL (4.94 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (4.94 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (4.94 mM); Clear solution

This protocol yields a clear solution of ≥ 3 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 (30.0 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 (sealed storage, away from moisture)

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: 99.65%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (254 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Kazi A, et al. Dual farnesyl and geranylgeranyl transferase inhibitor thwarts mutant KRAS-driven patient-derived pancreatic tumors. Clin Cancer Res. 2019 Jun 21. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.6482 mL	8.2409 mL	16.4818 mL	41.2045 mL
	5 mM	0.3296 mL	1.6482 mL	3.2964 mL	8.2409 mL
	10 mM	0.1648 mL	0.8241 mL	1.6482 mL	4.1204 mL
	15 mM	0.1099 mL	0.5494 mL	1.0988 mL	2.7470 mL
	20 mM	0.0824 mL	0.4120 mL	0.8241 mL	2.0602 mL
	25 mM	0.0659 mL	0.3296 mL	0.6593 mL	1.6482 mL
	30 mM	0.0549 mL	0.2747 mL	0.5494 mL	1.3735 mL
	40 mM	0.0412 mL	0.2060 mL	0.4120 mL	1.0301 mL
	50 mM	0.0330 mL	0.1648 mL	0.3296 mL	0.8241 mL
	60 mM	0.0275 mL	0.1373 mL	0.2747 mL	0.6867 mL
	80 mM	0.0206 mL	0.1030 mL	0.2060 mL	0.5151 mL
	100 mM	0.0165 mL	0.0824 mL	0.1648 mL	0.4120 mL