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  1. Vitamin D Related/Nuclear Receptor
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  3. SI-2 hydrochloride

SI-2 hydrochloride  (Synonyms: EPH 116 hydrochloride)

目錄號: HY-101447A 純度: 99.79%
COA 產(chǎn)品使用指南 技術(shù)支持

SI-2 (EPH 116 hydrochloride) 是 SRC-3 的抑制劑,誘導(dǎo)乳腺癌細(xì)胞死亡的 IC50 值為 3-20 nM。SI-2 (EPH 116 hydrochloride) 具有良好的藥代動力學(xué)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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規(guī)格 價格 是否有貨 數(shù)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 現(xiàn)貨 詢價
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Customer Review

Other Forms of SI-2 hydrochloride:

查看 Estrogen Receptor/ERR 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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].

體外研究
(In Vitro)

SI-2 hydrochloride 通過與SRC-3的直接物理相互作用選擇性降低細(xì)胞內(nèi)SRC-3的轉(zhuǎn)錄活性和蛋白濃度[1]。
SI-2 hydrochloride 選擇性誘導(dǎo)乳腺癌細(xì)胞死亡IC50 值在低納摩爾范圍 (3 -20 nM),但不影響正常細(xì)胞活力[1]
SI-2 hydrochloride (100 nM) 降低 MDAMB-468 細(xì)胞的細(xì)胞運(yùn)動、侵襲和腫瘤轉(zhuǎn)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.
體內(nèi)研究
(In Vivo)

根據(jù) hERG 通道阻斷試驗(yàn),SI-2 hydrochloride 引起的急性心臟毒性極小,根據(jù)組織學(xué)分析,SI-2 hydrochloride 對主要器官的慢性毒性微乎其微[1]。
SI-2 hydrochloride 是一種類藥分子并且滿足 Lipinski 規(guī)則的所有條件。[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 號
性狀

固體

顏色

Pink to red

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 5 mg/mL (16.57 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱:
SI-2 hydrochloride
目錄號:
HY-101447A
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