1. 疾病领域
  2. 癌症 泌尿生殖系统疾病
  3. 乳腺癌 前列腺癌 泌尿生殖系统癌症
  4. Anticancer agent 303

Anticancer agent 303 是一种选择性、口服有效的吡唑并吡啶衍生物类抗癌剂。Anticancer agent 303 对健康细胞毒性较低,在癌细胞与健康细胞间的选择窗口约为 2 倍。Anticancer agent 303 经腹腔或口服给药后,能在小鼠体内产生可检测的全身暴露量。Anticancer agent 303 能有效抑制前列腺癌和乳腺癌细胞的增殖。

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Anticancer agent 303

Anticancer agent 303 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anticancer agent 303 is a selective, orally active anticancer agent belonging to the pyrazolopyridine derivatives. Anticancer agent 303 exhibits low cytotoxicity to healthy cells, with a selective window of approximately 2-fold between cancer cells and healthy cells. Anticancer agent 303 produces detectable systemic exposure in mice following intraperitoneal or oral administration. Anticancer agent 303 effectively inhibits the proliferation of prostate cancer and breast cancer cells[1].

体外研究
(In Vitro)

Anticancer agent 303 (compound 17) (5 μM; 72 h) 可抑制 PC-3、MCF-7、HUVEC 细胞活力,平均 IC50 分别为 4.8 μM、3.9 μM、8.7 μM[1]
Anticancer agent 303 (5 μM; 1-24 h) 以时间依赖的方式在 PC-3 细胞内蓄积,经 5 μM 处理 24 h 后达到 245.8 ng/40,000 细胞 (为初始给药剂量的 104.5%)[1]

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

Cell Cytotoxicity Assay[1]

Cell Line: human prostate adenocarcinoma PC-3 cells
Concentration: 5 μM
Incubation Time: 72 h
Result: Reduced PC-3 cell viability to 36% relative to DMSO control.
Exhibited an average IC50 of 4.8 ± 0.9 μM.

Cell Cytotoxicity Assay[1]

Cell Line: human breast adenocarcinoma MCF-7 cells
Concentration: 5 μM
Incubation Time: 72 h
Result: Reduced MCF-7 cell viability to 33% relative to DMSO control.
Exhibited an average IC50 of 3.9 ± 0.9 μM.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 AUC0-t AUC0-∞ Bioavailability
Mice[1] 4 mg/kg i.p. 372.2 ng/mL 4.8 h 14.4 h 5847.1 ng·h/mL 8721.3 ng·h/mL /
Mice[1] 8 mg/kg p.o. 199.0 ng/mL 6.5 h 16.3 h 3338.0 ng·h/mL 5299.1 ng·h/mL 29.13 %
体内研究
(In Vivo)

Anticancer agent 303 (compound 17) 可通过腹腔和口服途径在小鼠体内产生全身暴露量,腹腔注射相比口服能产生更高的全身暴露量(表现为 Cmax 和 AUC 增加),且腹腔给药的达峰时间(Tmax)更短,但两种途径的消除半衰期相似。此外,Anticancer agent 303 的剂量归一化相对口服生物利用度为 29.13%[1]

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

分子量

470.57

Formula

C27H30N6O2

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 *
= × ×

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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Anticancer agent 303
目录号:
HY-181558
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