SI-2 hydrochloride_product_DataBase

Bioactivity	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].
Target	IC50：3-20 nM (breast cancer cell death).
Invitro	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]. Cell Viability Assay[1]. Cell Line:
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]. Animal Model:
Name	SI-2 hydrochloride
CAS	1992052-49-9
Formula	C15H16ClN5
Molar Mass	301.77
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Song X, et al. Development of potent small-molecule inhibitors to drug the undruggable steroid receptor coactivator-3. Proc Natl Acad Sci U S A. 2016 May 3;113(18):4970-5.

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