API-59CJ-Ome hydrate

• Catalog No.: A8979
• M. F.: C21H24N2O4
• M. W.: 368.42626
• Purity: ≥98% (HPLC)
• Storage: under inert gas

SYNONYMS

• IUPAC name: 9-methoxy-2,5,11-trimethyl-6H-pyrido[4,3-b]carbazol-2-ium acetate hydrate
• IUPAC Traditional name: 9-methoxy-2,5,11-trimethyl-6H-pyrido[4,3-b]carbazol-2-ium acetate hydrate
• Synonyms: 9-Methoxy-2-methylellipticinium acetate hydrate

DATABASE IDS

• EC Number: 308-789-6
• PubChem SID: 24724403
• MDL Number: MFCD08705317

PROPERTIES

• Empirical Formula (Hill Notation): C19H19N2O · C2H3O2 · xH2O
• Purity: ≥98% (HPLC)
• Apperance: red lyophilized powder
• Solubility: H2O: soluble1 mg/mL
• Solubility: DMSO: ≥2 mg/mL, clear, dark red (with 5 min sonication)
• GHS Signal Word: Warning
• GHS Hazard statements: H319
• Personal Protective Equipment: Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter
• GHS Precautionary statements: P305 + P351 + P338
• Storage Condition: under inert gas
• Storage Temperature: 2-8°C
• German water hazard class: 3

DETAILS

Description (English)

Biochem/physiol Actions
API-59CJ-Ome hydrate is a highly selective Akt/PKB inhibitor. The PTEN (phosphatase and tensin homolog deleted on chromosome 10) tumor suppressor is mutated in 40-50% of human endometrial cancers. PTEN exerts its effects in part via inhibition of the antiapoptotic protein AKT. The endometrial cancer cell lines that express PTEN mutations show high levels of phosphorylated AKT and high AKT kinase activity. The endometrial cancer cell lines that express wild-type PTEN have little phosphorylated AKT and AKT kinase activity. API-59CJ-OMe inhibits AKT kinase activity and induces apoptosis in the cell lines with high AKT activity, but has little effect on cells without AKT activity. API-59CJ-OMe may therefore have therapeutic potential for those endometrial cancers that harbor PTEN mutations and AKT activation.

Description (简体中文)

Biochem/physiol Actions
API-59CJ-Ome hydrate is a highly selective Akt/PKB inhibitor. The PTEN (phosphatase and tensin homolog deleted on chromosome 10) tumor suppressor is mutated in 40-50% of human endometrial cancers. PTEN exerts its effects in part via inhibition of the antiapoptotic protein AKT. The endometrial cancer cell lines that express PTEN mutations show high levels of phosphorylated AKT and high AKT kinase activity. The endometrial cancer cell lines that express wild-type PTEN have little phosphorylated AKT and AKT kinase activity. API-59CJ-OMe inhibits AKT kinase activity and induces apoptosis in the cell lines with high AKT activity, but has little effect on cells without AKT activity. API-59CJ-OMe may therefore have therapeutic potential for those endometrial cancers that harbor PTEN mutations and AKT activation.