GGTI-298 TRIFLUOROACETATE SALT HYDRATE (C005B-011817)

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
• to study its combinatorial effects with FTI-277 on statin-mediated activation of extracellular signal-regulated kinase 5 (ERK5) in the human endothelium
• to evaluate the effect of protein geranylgeranylation (GG) inhibition on the breast cancer stem cell (CSC) population

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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Molecular Weight: 593.66 (anhydrous basis). Empirical Formula: C₂₇H₃₃N₃O₃S · C₂HF₃O₂ · xH₂O. Quality Level: 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). Pictograms: GHS07. Signal Word: Warning. Hazard Statements: H315 - H319 - H335. Precautionary Statements: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338. Hazard Classifications: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3. Target Organs: Respiratory system. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable. Personal Protective Equipment: dust mask type N95 (US), Eyeshields, Gloves.