2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. Tubulin degrader 1

Tubulin degrader 1 (Compound 5i) 是 BML284 (HY-19987) 衍生物，是一种具有口服活性的秋水仙碱位点非共价微管蛋白降解剂，针对 5 种肿瘤细胞系 (Hela, HCT116, MCF-7, K562 and Molm-13) IC50 值为 0.02 - 0.05 μM。Tubulin degrader 1 具有抗增殖活性，可有效抑制肿瘤生长。

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Tubulin degrader 1 Chemical Structure

Tubulin degrader 1 Chemical Structure

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Tubulin degrader 1 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 degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth[1].

体外研究
(In Vitro)

Tubulin degrader 1 (0.2-25 μM, 24 h) 通过直接结合 Hela 细胞中的秋水仙碱位点发挥抗增殖活性[1]。
Tubulin degrader 1 (0-300 nM, 24 h) 可导致 A2780S 和 A2780T 细胞明显的 G2/M 期细胞周期停滞和细胞凋亡[1]。

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

Tubulin degrader 1 相关抗体:
体内研究
(In Vivo)

Tubulin degrader 1 (10-30 mg/kg, 静脉注射, 两天一次, 6-9 次) 在 A2780S 和 A2780T 异种移植模型中具有抗肿瘤活性[1]。

药代动力学分析[1]

Route Dose (mg/kg) T1/2 (h) Tmax (h) CLobs (L/h/kg) Vss (L/kg) AUC0-t (μg/mL*h) Cmax (μg/mL) F (%)
i.v. 10 1.93 0.08 2.55 7.43 4266.53 2885.77 -
p.o. 10 5.94 3.67 18.86 154.68 446.77 77.92 10.47

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

345.40

Formula

C20H19N5O
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 degrader 1 相关分类

  • 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.

Keywords:

Tubulin degrader 1Tubulin degrader1Tubulin degrader-1Microtubule/TubulinBML284antiproliferativetumorHelaHCT116MCF-7K562Molm-13A2780SA2780TInhibitorinhibitorinhibit

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目录号：
HY-161324
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