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

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].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780/Taxol IC50
16 nM
Compound: 5i
Antiproliferative activity against human A2780T cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human A2780T cells assessed as reduction in cell viability measured after 72 hrs
[PMID: 38430854]
A2780S IC50
18 nM
Compound: 5i
Antiproliferative activity against human A2780S cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human A2780S cells assessed as reduction in cell viability measured after 72 hrs
[PMID: 38430854]
A549 IC50
34 nM
Compound: 5i
Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs
[PMID: 38430854]
A549/TR IC50
37 nM
Compound: 5i
Antiproliferative activity against paclitaxel resistant human A549T cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against paclitaxel resistant human A549T cells assessed as reduction in cell viability measured after 72 hrs
[PMID: 38430854]
HCT-116 IC50
0.03 μM
Compound: 5i
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs
[PMID: 38430854]
HUVEC IC50
623 nM
Compound: 5i
Antivascular activity against human HUVEC cells assessed as inhibition of capillary tube formation incubated for 24 hrs by microscopy based analysis
Antivascular activity against human HUVEC cells assessed as inhibition of capillary tube formation incubated for 24 hrs by microscopy based analysis
[PMID: 38430854]
HeLa IC50
0.05 μM
Compound: 5i
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs
[PMID: 38430854]
K562 IC50
0.03 μM
Compound: 5i
Antiproliferative activity against human K562 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human K562 cells assessed as reduction in cell viability measured after 72 hrs
[PMID: 38430854]
MCF7 IC50
20 nM
Compound: 5i
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs
[PMID: 38430854]
MOLM-13 IC50
0.02 μM
Compound: 5i
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs
[PMID: 38430854]
NCI/ADR-RES IC50
32 nM
Compound: 5i
Antiproliferative activity against human MCF7ADR cells assessed as reduction in cell viability measured after 72 hrs
Antiproliferative activity against human MCF7ADR cells assessed as reduction in cell viability measured after 72 hrs
[PMID: 38430854]
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：
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