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FGTI-2734 - 99%, high purity , CAS No.1247018-19-4

COA

Grade & Purity:

≥99%

Cas Number: 1247018-19-4
Molecular Weight: 510.63
PubChem CID: 49783195

In stock

Item Number

F649320

Grouped product items
SKU	Size	Availability	Price
F649320-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$150.90
F649320-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$250.90
F649320-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$500.90
F649320-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$810.90
F649320-100mg	100mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,300.90

View related series

Amino Acid/Protein Metabolism (1836) Farnesyl Transferase (27) Metabolic Enzyme/Protease (4860)

Basic Description

Specifications & Purity	≥99%
Biochemical and Physiological Mechanisms	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 KR
Storage Temp	Store at 2-8°C
Shipped In	Wet ice This product requires cold chain shipping. Ground and other economy services are not available.
Product Description	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 tumors In Vitro FGTI-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 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 . 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:Solid IC50& Target:IC50: 250 nM (FT) and 520 nM (GGT-1)

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
- Superclass Organoheterocyclic compounds
  - Class Pyridines and derivatives
    - Subclass Pyridinesulfonamides

Kingdom	Organic compounds
Superclass	Organoheterocyclic compounds
Class	Pyridines and derivatives
Subclass	Pyridinesulfonamides
Intermediate Tree Nodes	Not available
Direct Parent	Pyridinesulfonamides
Alternative Parents	Dialkylarylamines Benzonitriles Aniline and substituted anilines Fluorobenzenes Aralkylamines Organosulfonamides N-substituted imidazoles Aryl fluorides Heteroaromatic compounds Aminosulfonyl compounds Nitriles Azacyclic compounds Organofluorides Organic oxides Hydrocarbon derivatives
Molecular Framework	Aromatic heteromonocyclic compounds
Substituents	Pyridine-2-sulfonamide - Benzonitrile - Dialkylarylamine - Aniline or substituted anilines - Fluorobenzene - Halobenzene - Aralkylamine - N-substituted imidazole - Monocyclic benzene moiety - Aryl fluoride - Benzenoid - Aryl halide - Organosulfonic acid amide - Heteroaromatic compound - Imidazole - Azole - Aminosulfonyl compound - Sulfonyl - Organosulfonic acid or derivatives - Organic sulfonic acid or derivatives - Tertiary amine - Azacycle - Carbonitrile - Nitrile - Hydrocarbon derivative - Organohalogen compound - Organofluoride - Amine - Organic nitrogen compound - Organonitrogen compound - Organosulfur compound - Organic oxygen compound - Cyanide - Organic oxide - Aromatic heteromonocyclic compound
Description	This compound belongs to the class of organic compounds known as pyridinesulfonamides. These are heterocyclic compounds containing a pyridine ring substituted by one or more sulfonamide groups.
External Descriptors	Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61. DOI: 10.1186/s13321-016-0174-y

Associated Targets(Human)

FNTA Tclin Protein farnesyltransferase (3470 Activities)

Discover Target: FNTA

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

FNTA Tclin Geranylgeranyl transferase type I (851 Activities)

Discover Target: FNTA

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mechanisms of Action

Mechanism of Action	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	References

Names and Identifiers

IUPAC Name	N-[2-[4-cyano-2-fluoro-N-[(3-methylimidazol-4-yl)methyl]anilino]ethyl]-N-(cyclohexylmethyl)pyridine-2-sulfonamide
INCHI	InChI=1S/C26H31FN6O2S/c1-31-20-29-17-23(31)19-32(25-11-10-22(16-28)15-24(25)27)13-14-33(18-21-7-3-2-4-8-21)36(34,35)26-9-5-6-12-30-26/h5-6,9-12,15,17,20-21H,2-4,7-8,13-14,18-19H2,1H3
InChIKey	BXNRVJLIEMQDOL-UHFFFAOYSA-N
Smiles	CN1C=NC=C1CN(CCN(CC2CCCCC2)S(=O)(=O)C3=CC=CC=N3)C4=C(C=C(C=C4)C#N)F
Isomeric SMILES	CN1C=NC=C1CN(CCN(CC2CCCCC2)S(=O)(=O)C3=CC=CC=N3)C4=C(C=C(C=C4)C#N)F
PubChem CID	49783195
Molecular Weight	510.63

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	DMSO : 50 mg/mL (97.92 mM; Need ultrasonic)
Molecular Weight	510.600 g/mol
XLogP3	4.000
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	10
Exact Mass	510.221 Da
Monoisotopic Mass	510.221 Da
Topological Polar Surface Area	104.000 Å²
Heavy Atom Count	36
Formal Charge	0
Complexity	839.000
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
The total count of all stereochemical bonds	0
Covalently-Bonded Unit Count	1

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