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SI-2 hydrochloride (Synonyms: EPH 116 hydrochloride)

Cat. No.: HY-101447A Purity: 98.12%
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SI-2 hydrochloride (EPH 116 hydrochloride) is a highly promising SRC-3 SMI: SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 hydrochloride (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability.

For research use only. We do not sell to patients.

SI-2 hydrochloride Chemical Structure

SI-2 hydrochloride Chemical Structure

CAS No. : 1992052-49-9

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Description

SI-2 hydrochloride (EPH 116 hydrochloride) is a highly promising SRC-3 SMI: SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 hydrochloride (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].

Cell Viability Assay[1].

Cell Line: MDA-MB-468 cells.
Concentration: 100 nM.
Incubation Time: 12 hours.
Result: Significantly reduced the motility of cancer cells.

Western Blot Analysis[1].

Cell Line: MDAMB-468 cells.
Concentration: 0-200 nM.
Incubation Time: 24 hours.
Result: Significantly reduced SRC-3 protein levels. Did not decrease the SRC-3 mRNA level.

Western Blot Analysis[1].

Cell Line: Cancer cells.
Concentration: 0-200 nM.
Incubation Time: 24 hours.
Result: Caused PARP cleavage.
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: MDA-MB-468 breast cancer mouse model[1].
Dosage: 2 mg/kg.
Administration: Twice daily for 5 weeks (Vehicle, PBS).
Result: Significantly inhibit tumor growth.
SRC-3 levels in SI-2–treated tumor tissues were significantly lower than the PBS treated control group.
Animal Model: CD1 mice[1].
Dosage: 20 mg/kg (Pharmacokinetic Analysis).
Administration: Intraperitoneal administration once.
Result: T1/2 = 1 h, Cmax of 3.0 μM, and the time to reach the maximum plasma concentration tmax of 0.25 h.
SI-2 only degrades slightly (less than 5%) at pH 1.6 and 3.0 within 6 h, and is stable in buffers with pH ≥ 5.
Molecular Weight

301.77

Formula

C₁₅H₁₆ClN₅

CAS No.

1992052-49-9

SMILES

CN1C(N/N=C(C)/C2=CC=CC=N2)=NC3=CC=CC=C13.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3138 mL 16.5689 mL 33.1378 mL
5 mM 0.6628 mL 3.3138 mL 6.6276 mL
10 mM 0.3314 mL 1.6569 mL 3.3138 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

SI-2EPH 116SI2SI 2EPH116EPH-116OthersPPIbreastcancerTNBCInhibitorinhibitorinhibit

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SI-2 hydrochloride
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