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SI-2 hydrochloride  (Synonyms: EPH 116 hydrochloride)

Cat. No.: HY-101447A Purity: 99.79%
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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.

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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Based on 1 publication(s) in Google Scholar

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SI-2 hydrochloride Related Antibodies

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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[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SI-2 hydrochloride Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

Pink to red

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (16.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3138 mL 16.5689 mL 33.1378 mL 82.8446 mL
5 mM 0.6628 mL 3.3138 mL 6.6276 mL 16.5689 mL
10 mM 0.3314 mL 1.6569 mL 3.3138 mL 8.2845 mL
15 mM 0.2209 mL 1.1046 mL 2.2092 mL 5.5230 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SI-21992052-49-9EPH 116SI2SI 2EPH116EPH-116OthersPPIbreastcancerTNBCInhibitorinhibitorinhibit

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