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FGTI-2734 mesylate (1247018-19-4 free base)

Catalog No. T11282LCas No. 2702297-24-1

FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.

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Pack Size	Price	Availability
5 mg	$311	Backorder
10 mg	$575	Backorder
50 mg	$1,762	Backorder
100 mg	$3,081	Backorder
200 mg	Inquiry	Backorder
500 mg	Inquiry	Backorder
1 mL x 10 mM (in DMSO)	$414	Backorder

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Product Introduction

Bioactivity

Description	FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.
In vitro	FGTI-2734 mesylate (3-30 μM;?72 hours) inhibits both protein prenylation of HDJ2, RAP1A, KRAS and NRAS. FGTI-2734 mesylate (1-30 μM; 72 hours) induces apoptosis in mutant KRAS-dependent, but not mutant KRAS- independent, human cancer cells. ??FGTI-2734 inhibits KRAS membrane localization in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells.
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.
Alias	FGTI-2734 mesylate

Chemical Properties

Molecular Weight	606.73
Formula	C27H35FN6O5S2
Cas No.	2702297-24-1

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 75 mg/mL (123.61 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6482 mL	8.2409 mL	16.4818 mL	82.4090 mL
5 mM	0.3296 mL	1.6482 mL	3.2964 mL	16.4818 mL
10 mM	0.1648 mL	0.8241 mL	1.6482 mL	8.2409 mL
20 mM	0.0824 mL	0.4120 mL	0.8241 mL	4.1204 mL
50 mM	0.0330 mL	0.1648 mL	0.3296 mL	1.6482 mL
100 mM	0.0165 mL	0.0824 mL	0.1648 mL	0.8241 mL

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

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