SI-2 Hydrochloride
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- CAS号:
- 1992052-49-9
- 英文名:
- SI-2 Hydrochloride
- 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
- 中文名:
- SI-2 Hydrochloride
- 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
- CBNumber:
- CB66113126
- 分子式:
- C15H16ClN5
- 分子量:
- 301.78
- MOL File:
- 1992052-49-9.mol
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SI-2 Hydrochloride性质、用途与生产工艺
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。
IC50：3-20 nM (breast cancer cell death).
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.
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Cell Line:
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MDA-MB-468 cells.
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Concentration:
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100 nM.
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Incubation Time:
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12 hours.
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Result:
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Significantly reduced the motility of cancer cells.
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Western Blot Analysis.
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Cell Line:
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MDAMB-468 cells.
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Concentration:
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0-200 nM.
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Incubation Time:
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24 hours.
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Result:
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Significantly reduced SRC-3 protein levels. Did not decrease the SRC-3 mRNA level.
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Western Blot Analysis.
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Cell Line:
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Cancer cells.
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Concentration:
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0-200 nM.
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Incubation Time:
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24 hours.
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Result:
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Caused PARP cleavage.
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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.
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Animal Model:
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MDA-MB-468 breast cancer mouse model.
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Dosage:
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2 mg/kg.
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Administration:
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Twice daily for 5 weeks (Vehicle, PBS).
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Result:
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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:
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CD1 mice.
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Dosage:
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20 mg/kg (Pharmacokinetic Analysis).
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Administration:
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Intraperitoneal administration once.
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Result:
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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.
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SI-2 Hydrochloride
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上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-101447A | SI-2 hydrochloride | | 1 mg | 500元 |
| 2024/04/30 | HY-101447A | SI-2 Hydrochloride
SI-2 hydrochloride | 1992052-49-9 | 5mg | 1100元 |
1992052-49-9, SI-2 Hydrochloride 相关搜索:
- C15H15N5HCl
- 1-甲基-2-(2-(1-(吡啶-2-基)亚乙基)肼基)-1H-苯并[D]咪唑盐酸盐
- 化合物SI-2盐酸盐
- 化合物 T12906
- 1992052-49-9
- 1-Methyl-2-(2-(1-(pyridin-2-yl)ethylidene)hydrazineyl)-1H-benzo[d]imidazole hydrochloride
- EPH 116 hydrochloride
- SI-2 Hydrochloride