SI-2 hydrochloride
Based on 1 Customer Validation
SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI). 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.
- Purity: 98.06%
- CAS No.: 1992052-49-9
- Formula: C15H16ClN5
- Molecular Weight:301.77
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50：3-20 nM (breast cancer cell death)[1].
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.
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Cell Line:MDA-MB-468 cells.
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Concentration:100 nM.
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Incubation Time:12 hours.
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Result:Significantly reduced the motility of cancer cells.
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Cell Line:MDAMB-468 cells.
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Concentration:0-200 nM.
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Incubation Time:24 hours.
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Result:Significantly reduced SRC-3 protein levels. Did not decrease the SRC-3 mRNA level.
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Cell Line:Cancer cells.
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Concentration:0-200 nM.
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Incubation Time:24 hours.
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Result:Caused PARP cleavage.
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.
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Animal Model:MDA-MB-468 breast cancer mouse model[1].
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Dosage:2 mg/kg.
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Administration:Twice daily for 5 weeks (Vehicle, PBS).
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Result:Significantly inhibit tumor growth.
SRC-3 levels in SI-2–treated tumor tissues were significantly lower than the PBS treated control group.
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Animal Model:CD1 mice[1].
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Dosage:20 mg/kg (Pharmacokinetic Analysis).
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Administration:Intraperitoneal administration once.
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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.
Chemical Information
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CAS No. 1992052-49-9
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Appearance Solid
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Molecular Weight 301.77
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Formula C15H16ClN5
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Color Pink to red
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SMILES
CN1C(N/N=C(C)/C2=CC=CC=N2)=NC3=CC=CC=C13.Cl
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Synonyms
EPH 116 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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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
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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 |
SI-2 hydrochloride Related Classifications
HY-101447A Related Classifications
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