1992052-49-9

中文名称 SI-2 Hydrochloride

英文名称 SI-2 Hydrochloride

CAS 1992052-49-9

分子式 C15H15N5·HCl

分子量 301.78

MOL 文件 1992052-49-9.mol

更新日期 2025/11/23 21:13:38

1992052-49-9 结构式

基本信息物理化学性质图谱信息 SI-2 Hydrochloride价格(试剂级) 常见问题列表

基本信息

中文别名

化合物SI-2盐酸盐
化合物 T12906
1-甲基-2-(2-(1-(吡啶-2-基)亚乙基)肼基)-1H-苯并[D]咪唑盐酸盐

英文别名

SI-2 Hydrochloride
EPH 116 hydrochloride
1-Methyl-2-(2-(1-(pyridin-2-yl)ethylidene)hydrazineyl)-1H-benzo[d]imidazole hydrochloride

物理化学性质

形态Solid

颜色Pink to red

图谱信息

SI-2 Hydrochloride(1992052-49-9)核磁图(¹HNMR)

SI-2 Hydrochloride价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2025/05/22	HY-101447A	SI-2 hydrochloride	1992052-49-9	1 mg	500元
2025/05/22	HY-101447A	SI-2 Hydrochloride SI-2 hydrochloride	1992052-49-9	5mg	1100元
2025/05/22	HY-101447A	SI-2 Hydrochloride SI-2 hydrochloride	1992052-49-9	10 mM * 1 mLin DMSO	1210元

常见问题列表

生物活性

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。

靶点

IC50：3-20 nM (breast cancer cell death).

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 IC ₅₀ 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.

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

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.

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.