2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Tubulin-IN-51

Tubulin-IN-51 是一种口服有效的微管蛋白 (Tubulin) 抑制剂 (IC50 = 31 nM)。Tubulin-IN-51 在体外促进微管蛋白聚合，不与 Paclitaxel (HY-B0015) 竞争性结合。Tubulin-IN-51 抑制 Vinblastine (HY-13780) 与微管蛋白的结合。Tubulin-IN-51 下调 G1 期细胞比例诱导细胞凋亡 (apoptosis)。Tubulin-IN-51 抑制多种裸鼠异种移植模型中的肿瘤生长。

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Tubulin-IN-51

Tubulin-IN-51 Chemical Structure

CAS No. : 849550-36-3

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Tubulin-IN-51 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

Tubulin-IN-51 is an orally available, potent tubulin inhibitor (IC50 = 31 nM). Tubulin-IN-51 promotes tubulin polymerization in vitro and does not compete with Paclitaxel (HY-B0015) for binding. Tubulin-IN-51 inhibits the binding of Vinblastine (HY-13780) to tubulin. Tubulin-IN-51 downregulates the proportion of cells in the G1 phase and induces apoptosis. Tubulin-IN-51 inhibits tumor growth in multiple nude mouse xenograft models[1].

体外研究
(In Vitro)

Tubulin-IN-51 (Compound 8) 促进微管蛋白聚合，这种现象类似于 Paclitaxel (HY-B0015) 的作用，并阻止 [3H] Vinblastine (HY-13780) 与微管蛋白结合[1]。

Tubulin-IN-51 在低化合物浓度 (10-35 nM) 下下调 G1 期细胞比例诱导细胞凋亡，在高化合物浓度 (35-200 nM) 下阻滞 G2/M 期，这种模式与Paclitaxel (HY-B0015) 的观察结果相似[1]。

Tubulin-IN-51 抑制 KB、KB 8.5 和 KBV1 细胞增殖，IC50 分别为 23 nM、67 nM 和 953 nM[1]。

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

Tubulin-IN-51 相关抗体:
体内研究
(In Vivo)

Tubulin-IN-51 (Compound 8) ( 15-20 mg/kg，静脉注射，分期后第 0、7、14 和 21 天) 可抑制肿瘤 (A549 NSCLC) 细胞异种移植小鼠模型中的肿瘤生长[1]。

Tubulin-IN-51 (2.5-50 mg/kg，口服，分期后第 0、7 天) 可抑制肿瘤 (U87-MG 人胶质母细胞瘤) 异种移植小鼠模型中的肿瘤生长[1]。

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

Animal Model: Tumor (A549 human NSCLC cells) (i.p., 1x106) xenograft mice model[1]
Dosage: 15 mg/kg, 20 mg/kg, 25 mg/kg
Administration: i.v. , on days 0, 7, 14, and 21 after tumor staging
Result: Inhibited tumor growth.
Animal Model: Tumor (U87-MG human glioblastoma) (i.p., 1x107) xenograft mice model[1]
Dosage: 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 25 mg/kg, 50 mg/kg on day 0 only
Administration: p.o., on days 0, 7 after tumor staging
Result: Inhibited tumor growth.
分子量

464.82

Formula

C18H18ClF5N6O
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

Tubulin-IN-51 相关分类

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  • 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:

Tubulin-IN-51849550-36-3Microtubule/TubulinApoptosisTubulin inhibitorKB cellKB 8.5 celland KBV1 cellTumor (A549 human NSCLC cells) xenograft mice modelTumor (U87-MG human glioblastoma) xenograft mice modelInhibitorinhibitorinhibit

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