产品
编 号：F246590
分子式：C15H16ClN5
分子量：301.77
分子式：C15H16ClN5
分子量：301.77
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1992052-49-9
产品详情
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.
体内研究：
根据 hERG 通道阻断试验，SI-2 hydrochloride 引起的急性心脏毒性极小，根据组织学分析，SI-2 hydrochloride 对主要器官的慢性毒性微乎其微。 SI-2 hydrochloride 是一种类药分子并且满足 Lipinski 规则的所有条件。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: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.
体外研究：
SI-2 hydrochloride 通过与SRC-3的直接物理相互作用选择性降低细胞内SRC-3的转录活性和蛋白浓度。 SI-2 hydrochloride 选择性诱导乳腺癌细胞死亡IC50 值在低纳摩尔范围 (3 -20 nM)，但不影响正常细胞活力。 SI-2 hydrochloride (100 nM) 降低 MDAMB-468 细胞的细胞运动、侵袭和肿瘤转移。
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.
体内研究：
根据 hERG 通道阻断试验，SI-2 hydrochloride 引起的急性心脏毒性极小，根据组织学分析，SI-2 hydrochloride 对主要器官的慢性毒性微乎其微。 SI-2 hydrochloride 是一种类药分子并且满足 Lipinski 规则的所有条件。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: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.
体外研究：
SI-2 hydrochloride 通过与SRC-3的直接物理相互作用选择性降低细胞内SRC-3的转录活性和蛋白浓度。 SI-2 hydrochloride 选择性诱导乳腺癌细胞死亡IC50 值在低纳摩尔范围 (3 -20 nM)，但不影响正常细胞活力。 SI-2 hydrochloride (100 nM) 降低 MDAMB-468 细胞的细胞运动、侵袭和肿瘤转移。
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