1. Neuronal Signaling Apoptosis
  2. Sigma Receptor Apoptosis Caspase
  3. SV119

SV119 是一种选择性 σ-2 受体 (σ₂ receptor) 配体 (Ki ≈ 5-10 nM)。SV119 通过激活 caspase-3 并促进线粒体去极化,诱导多种人类癌细胞系凋亡 (apoptosis)。SV119 可以增强 Paclitaxel (HY-B0015) 等化疗药物的作用,增强对肿瘤细胞的细胞毒性。SV119 在小鼠异种移植模型中单独使用或联合使用均可显著抑制肿瘤生长。SV119 可用于乳腺癌、前列腺癌和胰腺癌等癌症的研究。

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SV119

SV119 Chemical Structure

CAS No. : 913815-82-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SV119 is a selective sigma-2 (σ₂) receptor ligand (Ki ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer[1][2][3][4][5].

IC50 & Target[1]

Caspase 3

 

Caspase-7

 

体外研究
(In Vitro)

SV119 (0-10 µM) 可诱导 Panc1、CFPAC、ASPC、PancO2 细胞发生 caspase-3/7 依赖性凋亡[1]
SV119 对 sigma-2 受体的 EC50 在 MDA-MB-231 细胞中为 23.3 μM (最大细胞毒性 100%),在 MCF-7 细胞中为 17.6 μM (最大细胞毒性 100%)[2]
SV119 (30 µM, 24-48 小时) 可降低全长 Bid 的蛋白水平[2]
SV119 (0-10 µM, 24 小时) 可增加 ASPC-1、CFPAC、Panc1、PancO2 细胞的凋亡与 Gemcitabine (HY-17026) 和Paclitaxel (HY-B0015) 联合应用[4]
SV119 (10 mM,1.5 小时) 可降低 MDA-MB-435 细胞中癌症干细胞 (CSC) 的荧光[5]
SV119 (SV119-PEG-AuNC/DOX,覆盖密度 (50%)) 在 MDA-MB-435 细胞中与光热和化疗联合应用可显著减少乳腺细胞的形成和数量,并降低乳腺 CSC 的干细胞性[5]

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

Apoptosis Analysis[4]

Cell Line: Panc02 cells
Concentration: 0, 10 µM
Incubation Time: 24 h
Result: Induced apoptosis in cells that were both in G0 as well as in G1 to G2/S phase of the cell cycle in combination with Gemcitabine and Paclitaxel, with mean TUNEL-positivity ranged from 16.1% to 18.6% at 10 μM.
Increased mean TUNEL-positivity ranged from 26.5% to 70.5% in gemcitabine combination (50 nM) and from 26.6% to 53.8% in paclitaxel combination (50 nM).
Induced moderate apoptosis in Ki67 negative cells (G0 phase).
体内研究
(In Vivo)

SV119 (1 mg/只小鼠,腹腔注射,一次;每隔一天/每天,连续 7 天) 与 Gemcitabine 或 Paclitaxel 联合使用,可增加胰腺肿瘤 C57BL/6 小鼠模型中的细胞凋亡并减缓肿瘤生长[4]

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

Animal Model: Panc-02 (106) pancreatic tumors C57BL/6 mice (8-12 weeks old) model[4]
Dosage: 1 mg/mouse
Administration: i.p., once
Result: Increased apoptosis that were treated with conventional chemotherapy (Gemcitabine or Paclitaxel).
Animal Model: Panc-02 (106) pancreatic tumors C57BL/6 mice (8-12 weeks old) model[4]
Dosage: 1 mg/mouse and weekly gemcitabine (3 mg/mouse, i.p. for two weeks)/daily paclitaxel (0.3 mg/mouse, i.p. for 7 days)
Administration: i.p. every other day/daily, for 7 days
Result: Demonstrated a non significant tumor volume and survival advantage, significantly slowed tumor growth in combination with Gemcitabine and Paclitaxel.
分子量

403.56

Formula

C23H37N3O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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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SV119
目录号:
HY-177345
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