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SI-2 hydrochloride  (Synonyms: EPH 116 hydrochloride)

目录号: HY-101447A 纯度: 99.79%
COA 产品使用指南

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。

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SI-2 hydrochloride Chemical Structure

SI-2 hydrochloride Chemical Structure

CAS No. : 1992052-49-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1210
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1 mg ¥500
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5 mg ¥1100
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10 mg ¥1700
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50 mg ¥5500
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100 mg ¥8500
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Other Forms of SI-2 hydrochloride:

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

IC50:3-20 nM (breast cancer cell death)[1].

体外研究
(In Vitro)

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[1]
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[1]
SI-2 hydrochloride (100 nM) 降低 MDAMB-468 细胞的细胞运动、侵袭和肿瘤转移[1]

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

Cell Viability Assay[1].

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

Western Blot Analysis[1].

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[1].

Cell Line: Cancer cells.
Concentration: 0-200 nM.
Incubation Time: 24 hours.
Result: Caused PARP cleavage.
体内研究
(In Vivo)

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[1]
SI-2 hydrochloride 是一种类药分子并且满足 Lipinski 规则的所有条件。[1]

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

Animal Model: MDA-MB-468 breast cancer mouse model[1].
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[1].
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.
分子量

301.77

Formula

C15H16ClN5

CAS 号
性状

固体

颜色

Pink to red

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)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 5 mg/mL (16.57 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

SI-2 hydrochloride 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3138 mL 16.5689 mL 33.1378 mL 82.8446 mL
5 mM 0.6628 mL 3.3138 mL 6.6276 mL 16.5689 mL
10 mM 0.3314 mL 1.6569 mL 3.3138 mL 8.2845 mL
15 mM 0.2209 mL 1.1046 mL 2.2092 mL 5.5230 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
SI-2 hydrochloride
目录号:
HY-101447A
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