Art. -Nr.: HY-128350

FGTI-2734

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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

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Reinheit: 99.85%
CAS. Nr.: 1247018-19-4
Formel: C₂₆H₃₁FN₆O₂S
Molecular Weight:510.63

Speicherung:

4°C, stored under nitrogen

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

FGTI-2734 Chemical Structure

CAS. Nr.: 1247018-19-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
NIH3T3	IC₅₀	0.0887 μM Compound: 21b, FTI-2734	Inhibition of H-Ras farnesylation expressed in mouse NIH3T3 cells Inhibition of H-Ras farnesylation expressed in mouse NIH3T3 cells	[PMID: 20822181]
NIH3T3	IC₅₀	2.7 μM Compound: 21b, FTI-2734	Inhibition of Rap1A geranylgeranylation expressed in mouse NIH3T3 cells Inhibition of Rap1A geranylgeranylation expressed in mouse NIH3T3 cells	[PMID: 20822181]

In Vitro

FGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells^[1].
FGTI-2734 (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 and Calu6 cells
Concentration:

1, 3, 10, 30 μM
Incubation Time:

72 hours
Result:

Induced CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells.

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 (intraperitoneally; 100 mg/kg/daily 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.

Chemical Information

CAS. Nr. 1247018-19-4
Appearance Solid
Molecular Weight 510.63
Formel C₂₆H₃₁FN₆O₂S
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen

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

Publications (1)

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Journal Impact Factor

J Alzheimers Dis

Regulation of glial ApoE secretion by the mevalonate pathway is independent of ApoE isoform. [Abstract]

2025 Mar;104(2):473-487. PMID: 39994996

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (97.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9584 mL

9.7918 mL

19.5837 mL

5 mM

0.3917 mL

1.9584 mL

3.9167 mL

10 mM

0.1958 mL

0.9792 mL

1.9584 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 90% Corn Oil

Solubility: ≥ 7.5 mg/mL (14.69 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 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 (75.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9584 mL	9.7918 mL	19.5837 mL	48.9591 mL
	5 mM	0.3917 mL	1.9584 mL	3.9167 mL	9.7918 mL
	10 mM	0.1958 mL	0.9792 mL	1.9584 mL	4.8959 mL
	15 mM	0.1306 mL	0.6528 mL	1.3056 mL	3.2639 mL
	20 mM	0.0979 mL	0.4896 mL	0.9792 mL	2.4480 mL
	25 mM	0.0783 mL	0.3917 mL	0.7833 mL	1.9584 mL
	30 mM	0.0653 mL	0.3264 mL	0.6528 mL	1.6320 mL
	40 mM	0.0490 mL	0.2448 mL	0.4896 mL	1.2240 mL
	50 mM	0.0392 mL	0.1958 mL	0.3917 mL	0.9792 mL
	60 mM	0.0326 mL	0.1632 mL	0.3264 mL	0.8160 mL
	80 mM	0.0245 mL	0.1224 mL	0.2448 mL	0.6120 mL

Keywords

FGTI-2734

1 Cited Publications

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FGTI-2734

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) FGTI-2734

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

FGTI-2734

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) FGTI-2734

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

FGTI-2734 Related Classifications

HY-128350 Related Classifications