SI-2 hydrochloride(Synonyms: EPH 116 hydrochloride)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SI-2 hydrochloride (Synonyms: EPH 116 hydrochloride) 纯度: 98.12%

SI-2 (EPH 116 hydrochloride) 是 SRC-3 的抑制剂,诱导乳腺癌细胞死亡的 IC50 值为 3-20 nM。SI-2 (EPH 116 hydrochloride) 具有良好的药代动力学特征和改善的毒性,以及可接受的口服可用性。

SI-2 hydrochloride(Synonyms: EPH 116 hydrochloride)

SI-2 hydrochloride Chemical Structure

CAS No. : 1992052-49-9

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10 mM * 1 mL in DMSO ¥1210 In-stock
5 mg ¥1100 In-stock
10 mg ¥1700 In-stock
50 mg ¥5500 In-stock
100 mg ¥8500 In-stock
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SI-2 hydrochloride 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Anti-Breast Cancer Compound Library
  • Targeted Diversity Library

生物活性

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].

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(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].

上海金畔生物科技有限公司 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.

分子量

301.77

Formula

C15H16ClN5

CAS 号

1992052-49-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

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

配制储备液
浓度 溶剂体积 质量 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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Song X, et al. Development of potent small-molecule inhibitors to drug the undruggable steroid receptor coactivator-3. Proc Natl Acad Sci U S A. 2016 May 3;113(18):4970-5.

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