1. Immunology/Inflammation Apoptosis Metabolic Enzyme/Protease
  2. Aryl Hydrocarbon Receptor Apoptosis Caspase Cytochrome P450
  3. ZSTK3744 hydrochloride

ZSTK3744 hydrochloride 是一种芳香烃受体 (AhR) 激动剂。ZSTK3744 hydrochloride 可直接结合 AhR,上调包括 CYP1A1CYP1B1 TIPARP 在内的 AhR 靶基因的表达,并在三阴性乳腺癌细胞中介导细胞生长抑制活性。ZSTK3744 hydrochloride 可诱导三阴性乳腺癌细胞凋亡 (apoptosis)。ZSTK3744 hydrochloride 表现出抗肿瘤活性,可用于化疗耐药性三阴性乳腺癌的研究。

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ZSTK3744 hydrochloride

ZSTK3744 hydrochloride Chemical Structure

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Other Forms of ZSTK3744 hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZSTK3744 hydrochloride is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 hydrochloride directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 hydrochloride induces apoptosis in triple-negative breast cancer cells. ZSTK3744 hydrochloride exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer[1].

体外研究
(In Vitro)

ZSTK3744 (0.1-1000 nM; 72 h) (compound 12) hydrochloride 可强效抑制 MDA-MB-468 三阴性乳腺癌 (TNBC) 细胞的生长, IC50 为 0.87 nM[1]
ZSTK3744 (0.1-1000 nM; 72 h) hydrochloride 可强效抑制阿霉素耐药性 MDA-MB-468/AR 三阴性乳腺癌 (TNBC) 细胞的生长,IC50 为 0.92 nM[1]
ZSTK3744 (0.1-1000 nM; 72 h) hydrochloride 可抑制 Paclitaxel (HY-B0015) 耐药性 MDA-MB-468/PR 三阴性乳腺癌 (TNBC) 细胞的生长,IC50 为 23.54 nM[1]
ZSTK3744 (1-24 h) hydrochloride 可时间依赖性地上调 MDA-MB-468 三阴性乳腺癌 (TNBC) 细胞中 CYP1A1 和 TIPARP 的 mRNA 表达,处理后 1 小时起即可观察到显著的诱导作用[1]
ZSTK3744 (24 h) hydrochloride 可诱导 MDA-MB-468 TNBC 细胞发生细胞凋亡,其细胞生长抑制活性至少部分通过 caspase 依赖的凋亡通路介导[1]
ZSTK3744 (0.1-1000 nM; 72 h) hydrochloride 可强效抑制 MDA-MB-453 三阴性乳腺癌 (TNBC) 细胞的生长,IC50 为 1.14 nM[1]
ZSTK3744 (0.1-1000 nM; 72 h) hydrochloride 可强效抑制 DU4475 三阴性乳腺癌 (TNBC) 细胞的生长,IC50 小于 0.50 nM[1]
ZSTK3744 (0.1-1000 nM; 72 h) hydrochloride 对 Hs578T TNBC 细胞的生长无显著抑制作用,IC50 >500 nM[1]

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

Cell Viability Assay[1]

Cell Line: MDA-MB-453 TNBC cells
Concentration: 0.1, 1, 10, 100 and 10,000 nM
Incubation Time: 72 h
Result: Inhibited cell growth with an IC50 of 1.14 nM.
体内研究
(In Vivo)

ZSTK3744 (2.5-10 mg/kg; i.v.; on days 0, 7, and 14) hydrochloride 在阿霉素耐药三阴性乳腺癌 (TNBC) 小鼠异种移植模型中可产生显著的、剂量依赖性的肿瘤生长抑制作用[1]
ZSTK3744 (1-5 mg/kg; i.v.; on days 0, 4, and 8) hydrochloride 在亲本三阴性乳腺癌 (TNBC) 小鼠异种移植模型中抑制肿瘤生长[1]

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

Animal Model: NOD.CB17-Prkdcscid/J (NOD/SCID) (female, 6 weeks old, subcutaneous xenograft of adriamycin-resistant MDA-MB-468 cells)[1]
Dosage: 2.5 mg/kg; 10 mg/kg
Administration: i.v.; days 0, 7, 14
Result: Inhibited tumor growth in a dose-dependent manner.
Reduced tumor volume significantly compared with the vehicle-treated group and the eribulin-treated group.
Caused no significant effect on mouse body weight.
Animal Model: NOD.CB17-Prkdcscid/J (NOD/SCID) (female, 6 weeks old, subcutaneous xenograft of parental MDA-MB-468 cells)[1]
Dosage: 1 mg/kg; 2.5 mg/kg; 5 mg/kg
Administration: i.v.; days 0, 4, 8
Result: Reduced tumor volume at 2.5 and 5 mg/kg.
Reduced tumor volume relative to the vehicle-treated group at all tested doses, with the highest dose showing the greatest inhibition.
分子量

417.89

Formula

C22H20ClN7

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:
ZSTK3744 hydrochloride
目录号:
HY-181629A
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