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FGTI-2734

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COA HPLC HNMR

FGTI-2734

Catalog No. T11282Cas No. 1247018-19-4

FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors.

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Pack Size	Price	Availability
1 mg	$47	In Stock
5 mg	$122	In Stock
10 mg	$198	In Stock
25 mg	$413	In Stock
50 mg	$618	In Stock
100 mg	$879	In Stock
1 mL x 10 mM (in DMSO)	$138	In Stock

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Product Introduction

Bioactivity

Description	FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors.
Targets&IC50	FTase:250 nM , GGTase I:520 nM
In vitro	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. FGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells.
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.

Chemical Properties

Molecular Weight	510.63
Formula	C26H31FN6O2S
Cas No.	1247018-19-4

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 50 mg/mL (97.92 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9584 mL	9.7918 mL	19.5837 mL	97.9183 mL
5 mM	0.3917 mL	1.9584 mL	3.9167 mL	19.5837 mL
10 mM	0.1958 mL	0.9792 mL	1.9584 mL	9.7918 mL
20 mM	0.0979 mL	0.4896 mL	0.9792 mL	4.8959 mL
50 mM	0.0392 mL	0.1958 mL	0.3917 mL	1.9584 mL

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