SI-2 hydrochloride 是 Src-3 的抑制剂，诱导乳腺癌细胞死亡的 IC50 值为 3-20 nM。SI-2 hydrochloride 具有良好的药代动力学特征和改善的毒性，以及可接受的口服可用性。

SI-2 hydrochloride is a highly promising inhibitor of SRC-3 SMI: SRC-3 (PPI)(IC50 values of 3-20 nM for breast cancer cell death), with acceptable oral availability.

SI-2 selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells through direct physical interactions with SRC-3. Breast cancer cell death selectively induced by SI-2 with IC50 of 3-20 nM. SI-2 (100 nM) decreases cell motility, invasion, and tumor metastasis in MDAMB-468 cells[1].

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. SI-2 is a drug-like molecule and meets all of the criteria of Lipinski’s rule[1].

1992052-49-9

C15H16ClN5

301.77

EPH 116 hydrochloride

DMSO:4.5mg/mL (14.9mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years