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About This Item
Empirical Formula (Hill Notation):
C19H13F7N2O2
CAS Number:
Molecular Weight:
434.31
UNSPSC Code:
12352200
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
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.
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