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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.06%
- CAS 番号: 1992052-49-9
- 分子式: C15H16ClN5
- 分子量:301.77
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保管条件:
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
化学情報
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CAS 番号 1992052-49-9
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性状 Solid
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分子量 301.77
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分子式 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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別名
EPH 116 hydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-101447A 関連分類
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