Description
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.
Product information
CAS Number: 1992052-49-9
Molecular Weight: 301.77
Formula: C15H16ClN5
Chemical Name: 1-methyl-2-[(E)-2-[1-(pyridin-2-yl)ethylidene]hydrazin-1-yl]-1H-1,3-benzodiazole hydrochloride
Smiles: Cl.C/C(=N\NC1=NC2=CC=CC=C2N1C)/C1=CC=CC=N1
InChiKey: CDYJHORKRVKALB-NWBUNABESA-N
InChi: InChI=1S/C15H15N5.ClH/c1-11(12-7-5-6-10-16-12)18-19-15-17-13-8-3-4-9-14(13)20(15)2;/h3-10H,1-2H3,(H,17,19);1H/b18-11+;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 5 mg/mL (16.57 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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. SI-2 (100 nM) decreases cell motility, invasion, and tumor metastasis in MDAMB-468 cells.
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. SI-2 is a drug-like molecule and meets all of the criteria of Lipinski’s rule.
Products are for research use only. Not for human use.
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