SI-2 (hydrochloride)

1992052-49-9

301.77

DMSO : 5 mg/mL (16.57 mM; Need ultrasonic)

Others

SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI), with IC₅₀ values of 3-20 nM for breast cancer cell death. SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability^[1]. IC50 & Target: IC50:3-20 nM (breast cancer cell death)^[1]. In Vitro: SI-2 selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells through direct physical interactions with SRC-3^[1].
SI-2 selectively induces breast cancer cell death with IC₅₀ values in the low nanomolar range (3-20 nM), but not affect normal cell viability^[1].
SI-2 (100 nM) decreases cell motility, invasion, and tumor metastasis in MDAMB-468 cells^[1].
In Vivo: SI-2 causes minimal acute cardiotoxicity based on a hERG channel blocking assay and an unappreciable chronic toxicity to major organs based on histological analyses^[1].
SI-2 is a drug-like molecule and meets all of the criteria of Lipinski's rule^[1].