2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. Anticancer agent 98

Anticancer agent 98 (compound 12k) 是微管蛋白聚合抑制剂 (Kd=16.9 μM)。Anticancer agent 98 对肿瘤细胞发挥抗增殖作用，在体外表现出抗血管生成作用。Anticancer agent 98 表现出良好的人和小鼠肝微粒体稳定性，t1/2>300 分钟。

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Anticancer agent 98 Chemical Structure

Anticancer agent 98 Chemical Structure

CAS No. : 2857070-72-3

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Anticancer agent 98 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min[1].

体外研究
(In Vitro)

Anticancer agent 98 抑制黑色素瘤、乳腺癌和胰腺癌的癌症增殖，IC50 范围为 0.6-3 nM[1]。
Anticancer agent 98 (300 nM、1 μM 或 3 μM；2 小时) 剂量依赖性地增加 PC-3 细胞中的 β-微管蛋白加合物[1]。
Anticancer agent 98 (3.125、6.25、12.5、25 和 50 μM) 对微管蛋白具有高结合亲和力，SPR 光谱分析的 Kd 值为 16.9 μM[1]。
Anticancer agent 98 (10 μM、50 μM；0-60 分钟) 在 60 分钟内强烈抑制微管蛋白聚合[1]。
Anticancer agent 98 (100 nM; 4 h) 在体外对 COS-7 细胞具有抗增殖和抗血管生成作用[1]。

体外代谢稳定性[1]

human microsomes mouse microsomes
t1/2 (min) CLint (μL/min/mg) t1/2 (min) CLint (μL/min/mg)
>300 <2.31 >300 <2.31

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

Anticancer agent 98 相关抗体:
体内研究
(In Vivo)

Anticancer agent 98 (2.5 mg/kg；静脉注射；每周两次，持续 2 周) 耐受性良好，在雄性 NSG 小鼠的 PC3/TxR 异种移植肿瘤中没有显着的体重减轻。相对于 Paclitaxel (HY-B0015；10 mg/kg，每周一次) 和对照组，Anticancer agent 98 还显着减缓了前列腺癌肿瘤的进展[1]。

NSG 小鼠中的药代动力学分析[1]

Route Dose (mg/kg) Cmax (ng/mL) tmax (min) AUC (ng·min/mL) t1/2 (min) F (%)
i.v. 4 1247 5.0 173,476 238 /
p.o. 10 78.3 10.0 8161 358 2.02

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

Animal Model: PC3/TxR xenograft model in NSG mouse[1]
Dosage: 2.5 mg/kg
Administration: IV; twice weekly for 2 weeks
Result: Inhibited the tumor growth in volume by approximately 85.6%. And inhibited angiogenesis by 44% related to control group.
Overcame taxane resistance at a low, safe, but potent dose in vivo.
分子量

325.37

Formula

C17H19N5O2
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

Anticancer agent 98 相关分类

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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.

Keywords:

Anticancer agent 982857070-72-3Anticancer agent98Anticancer agent-98Microtubule/TubulinInhibitorinhibitorinhibit

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