SI-2 Hydrochloride

生物活性靶点体外研究体内研究 SI-2 Hydrochloride 试剂级价格

SI-2 Hydrochloride

CAS号:1992052-49-9
英文名:SI-2 Hydrochloride
中文名:SI-2 Hydrochloride
CBNumber:CB66113126
分子式:C15H16ClN5
分子量:301.78
MOL File:1992052-49-9.mol

SI-2 Hydrochloride化学性质

形态 :Solid
颜色 :Pink to red

SI-2 Hydrochloride性质、用途与生产工艺

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.