FGTI-2734

FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC 50 s 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 tumorsIn VitroFGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell 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 AnalysisCell 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 VivoFGTI-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 . 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 Dosage: 100 mg/kg Administration: Intraperitoneally; daily; for 18 to 25 days Result: Inhibited tumor growth in mutant KRAS-dependent tumors.Form:SolidIC50& Target:IC50: 250 nM (FT) and 520 nM (GGT-1)

Specifications & Purity: FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC 50 s 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 tumorsIn VitroFGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell 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 AnalysisCell 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 VivoFGTI-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 . 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 Dosage: 100 mg/kg Administration: Intraperitoneally; daily; for 18 to 25 days Result: Inhibited tumor growth in mutant KRAS-dependent tumors.Form:SolidIC50& Target:IC50: 250 nM (FT) and 520 nM (GGT-1)

Grade: Moligand™

Molecular Formula: C26H31FN6O2S

Molecular Weight: 510.63

PubChem CID: 49783195

Isomeric SMILES: CN1C=NC=C1CN(CCN(CC2CCCCC2)S(=O)(=O)C3=CC=CC=N3)C4=C(C=C(C=C4)C#N)F

Storage Temperature: Store at -20°C;Argon charged

Shipped in: Ice chest + Ice pads

UPC:

51442306

Weight:

1.06 Ounces

HazmatClass:

Yes

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

F649320-1mg

Country of Origin:

China

CAS:

1247018-19-4

Product Size:

1mg

Harmonized Tariff Code:

2931.90.90