SI-2 hydrochloride EPH 116 hydrochloride|cas:1992052-49-9|西域试剂

SI-2 hydrochloride EPH 116 hydrochloride,99.79%

产品编号：Bellancom-101447A| CAS NO：1992052-49-9| 分子式：C₁₅H₁₆ClN₅| 分子量：301.77

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货号	价格	库存与货期
Bellancom-101447A	￥1100.00	杭州北京（现货）
Bellancom-101447A	￥1700.00	杭州北京（现货）
Bellancom-101447A	￥5500.00	杭州北京（现货）
Bellancom-101447A	￥8500.00	杭州北京（现货）

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SI-2 hydrochloride EPH 116 hydrochloride

产品介绍

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。

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.

体外研究

SI-2 selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells through direct physical interactions with SRC-3.
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.
SI-2 (100 nM) decreases cell motility, invasion, and tumor metastasis in MDAMB-468 cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay.

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

Western Blot Analysis.

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.

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.
SI-2 is a drug-like molecule and meets all of the criteria of Lipinski’s rule.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	MDA-MB-468 breast cancer mouse model.
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.
Dosage:	20 mg/kg (Pharmacokinetic Analysis).
Administration:	Intraperitoneal administration once.
Result:	T_1/2 = 1 h, C_max of 3.0 μM, and the time to reach the maximum plasma concentration t_max 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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	MDA-MB-468 breast cancer mouse model.
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.
Dosage:	20 mg/kg (Pharmacokinetic Analysis).
Administration:	Intraperitoneal administration once.
Result:	T_1/2 = 1 h, C_max of 3.0 μM, and the time to reach the maximum plasma concentration t_max 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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	MDA-MB-468 breast cancer mouse model.
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.
Dosage:	20 mg/kg (Pharmacokinetic Analysis).
Administration:	Intraperitoneal administration once.
Result:	T_1/2 = 1 h, C_max of 3.0 μM, and the time to reach the maximum plasma concentration t_max 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.

性状

Solid

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。

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)

参考文献