SML4348

ErSO-TFPy

≥98% (HPLC)

• Synonym(e): (R)-3-(4-Hydroxyphenyl)-3-(3,3,4,4-tetrafluoropyrrolidin-1-yl)-7-(trifluoromethyl)indolin-2-one, (3R)-1,3-dihydro-3-(4-hydroxyphenyl)-3-(3,3,4,4-tetrafluoro-1-pyrrolidinyl)-7-(trifluoromethyl)-2H-Indol-2-one, R-26
• Empirische Formel (Hill-System): C₁₉H₁₃F₇N₂O₂
• CAS-Nummer: 3035547-78-2
• Molekulargewicht: 434.31
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Beschreibung

Biochem/physiol Actions

ErSO-TFPy potently inhibits multiple ERα+ breast cancer cell lines, exhibiting nanomolar IC50 values (≈ 5-25 nM). Its mechanism of action involves cation dysregulation, leading to cell swelling and the rapid induction of TRPM4-dependent necrotic cell death via activation of the anticipatory Unfolded Protein Response (a-UPR). Remarkably, a single dose of ErSO-TFPy achieves complete regressions of large tumors in preclinical models with sustained effect, despite its short half-life and transient blood exposure. This single-dose efficacy is coupled with excellent tolerability, demonstrated by high maximum tolerated doses (MTD) in mice (150 mg/kg IV), rats (>50 mg/kg IV), and dogs (>5 mg/kg IV), and a favorable therapeutic index, contrasting with multi-dose requirements of typical chemotherapies.

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• Gefahrencodes: H302,H315
• Sicherheitshinweise: P264 - P280 - P301 + P312 - P302 + P352 - P332 + P313 - P362 + P364
• Hazard Classifications: Acute Tox. 4 Oral - Skin Irrit. 2
• Lagerklasse: 11 - Combustible Solids
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable