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

Catalog No. T11282L CAS 2702297-24-1

Synonyms: FGTI-2734 mesylate

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

FGTI-2734 mesylate (1247018-19-4 free base), CAS 2702297-24-1

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5 mg	Inquiry	$ 311.00
10 mg	Inquiry	$ 575.00
50 mg	Inquiry	$ 1,762.00
100 mg	Inquiry	$ 3,081.00
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1 mL * 10 mM (in DMSO)	Inquiry	$ 414.00

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Biological Description

Chemical Properties

Storage & Solubility Information

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.
Targets&IC50	GGT:520 nM , FT:250 nM
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.

Synonyms	FGTI-2734 mesylate
Molecular Weight	606.73
Formula	C27H35FN6O5S2
CAS No.	2702297-24-1

Storage

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

Solubility Information

DMSO: 75 mg/mL (123.61 mM), Sonication is recommended.

References and Literature

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.

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Keywords

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