G5169

GGTI 298 trifluoroacetate salt hydrate

≥90% (HPLC), film

• Synonym(e): N-[[4-(2-(R)-Amino-3-mercaptopropyl)amino]-2-naphthylbenzoyl]leucine methyl ester trifluoroacetate salt hydrate
• Empirische Formel (Hill-System): C₂₇H₃₃N₃O₃S · C₂HF₃O₂ · xH₂O
• CAS-Nummer: 1217457-86-7
• Molekulargewicht: 593.66 (anhydrous basis)
• NACRES: NA.77
• PubChem Substance ID: 24724490
• UNSPSC Code: 51111800
• MDL number: MFCD06409252
• Assay: ≥90% (HPLC)
• Form: film, lyophilized

Eigenschaften

• Quality Segment: 100
• assay: ≥90% (HPLC)
• form: film, lyophilized
• impurities: <10% dimer
• color: colorless
• mp: 99.5-100 °C
• solubility: DMSO: >20 mg/mL
• storage temp.: −20°C
• SMILES string: OC(=O)C(F)(F)F.COC(=O)[C@H](CC(C)C)NC(=O)c1ccc(NC[C@@H](N)CS)cc1-c2cccc3ccccc23
• InChI: 1S/C27H33N3O3S.C2HF3O2/c1-17(2)13-25(27(32)33-3)30-26(31)23-12-11-20(29-15-19(28)16-34)14-24(23)22-10-6-8-18-7-4-5-9-21(18)22;3-2(4,5)1(6)7/h4-12,14,17,19,25,29,34H,13,15-16,28H2,1-3H3,(H,30,31);(H,6,7)/t19-,25+;/m1./s1
• InChI key: WALKWJPZELDSKT-UFABNHQSSA-N
• Gene Information: human ... PGGT1B(5229)

Beschreibung

Application

GGTI 298 trifluoroacetate salt hydrate has been used as a geranylgeranyltransferase I (GGTase I) inhibitor:

• to study the anticancer effects of statins along with GGTI 298[1]
• to study its combinatorial effects with FTI-277 on statin-mediated activation of extracellular signal-regulated kinase 5 (ERK5) in the human endothelium[2]
• to evaluate the effect of protein geranylgeranylation (GG) inhibition on the breast cancer stem cell (CSC) population[3]

Biochem/physiol Actions

GGTI 298 is a cell-permeable, prodrug form of the geranylgeranyltransferase I (GGTase I) inhibitor GGTI-297. It inhibits the processing of Rap 1A without effecting the processing of H-Ras.

Features and Benefits

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Sicherheitshinweise

• pictograms: GHS07
• signalword: Warning
• hcodes: H315,H319,H335
• pcodes: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Hazard Classifications: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• target_organs: Respiratory system
• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable
• ppe: dust mask type N95 (US), Eyeshields, Gloves