2. PROTAC Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. PROTACs Microtubule/Tubulin Apoptosis
  4. PROTAC tubulin-Degrader-1

PROTAC tubulin-Degrader-1 是一种 α/β/β3-tubulin PROTAC 降解剂。PROTAC tubulin-Degrader-1 对多种人类肿瘤细胞系表现出强效的抗增殖活性。PROTAC tubulin-Degrader-1 可诱导 A549 和 A549/Taxol 细胞的 G2/M 期阻滞和凋亡 (apoptosis)，并抑制其集落形成。PROTAC tubulin-Degrader-1 在 A549 和 A549/Taxol 异种移植瘤模型中显示出显著的抗肿瘤功效。PROTAC tubulin-Degrader-1 可用于非小细胞肺癌 (NSCLC) 的相关研究。(粉色：Tubulin 配体 (HY-N2146), 蓝色：CRBN 配体 (HY-10984), 黑色：连接子 (HY-N6056))。

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PROTAC tubulin-Degrader-1

PROTAC tubulin-Degrader-1 Chemical Structure

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PROTAC tubulin-Degrader-1 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056))[1].

IC50 & Target[1]

Cereblon

 

α-tubulin

296 nM (DC50, A549 cells)

α-tubulin

32 nM (DC50, A549/Taxol cells)

β-tubulin

856 nM (DC50, A549 cells)

β-tubulin

972 nM (DC50, A549/Taxol cells)

β3-tubulin

251 nM (DC50, A549 cells)

β3-tubulin

5 nM (DC50, A549/Taxol cells)

体外研究
(In Vitro)

PROTAC tubulin-Degrader-1 (Compound W13) (4-21 nM, 72 h) 对多种人类肿瘤细胞系 (MCF-7, A549, HepG2, MGC-803, HeLa, U937) 表现出强大的抗增殖活性，IC50 值范围为 0.004 μM 至 0.021 μM[1]。
PROTAC tubulin-Degrader-1 (0-1.25 μM, 48 h) 有效降解 α-tubulin (DC50 = 296 nM in A549, DC50 = 32 nM in A549/Taxol)、β-tubulin (DC50 = 856 nM in A549, DC50 = 972 nM in A549/Taxol) 并强效降解 β3-tubulin (DC50 = 251 nM in A549, DC50 = 5 nM in A549/Taxol)[1]。
PROTAC tubulin-Degrader-1 (0.25 μM, 24-48 h) 通过泛素-蛋白酶体系统 (UPS) 诱导微管蛋白降解[1]。
PROTAC tubulin-Degrader-1 (2-50 nM, 24-48 h) 以剂量依赖性方式诱导 A549 和 A549/Taxol 细胞的 G2/M 期阻滞并促进细胞凋亡[1]。
PROTAC tubulin-Degrader-1 (2-50 nM, 14 days) 以剂量依赖性方式抑制 A549 和 A549/Taxol 细胞的集落形成[1]。
PROTAC tubulin-Degrader-1 (2.5-10 nM, 6-8 h) 强烈抑制人脐静脉内皮细胞 (HUVECs) 在 Matrigel 上的管形成，以剂量依赖性方式减少节点数、主连接数、线段长度、总分支长度和网孔数[1]。

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

PROTAC tubulin-Degrader-1 相关抗体:

Cell Cycle Analysis[1]

Cell Line: A549 and A549/Taxol cells
Concentration: 2, 10, 50 nM
Incubation Time: 24 h
Result: Induced G2/M phase arrest in A549 and A549/Taxol cells in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: A549 and A549/Taxol cells
Concentration: 2, 10, 50 nM
Incubation Time: 48 h
Result: Induced apoptosis in A549 and A549/Taxol cells in a dose-dependent manner.
体内研究
(In Vivo)

PROTAC tubulin-Degrader-1 (Compound W13) (15 mg/kg，腹腔注射，每两天一次，23 天) 在 A549 和 A549/Taxol (耐紫杉醇) 异种移植模型中表现出强大的抗肿瘤效能[1]。

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

Animal Model: A549 cells or A549/Taxol cells (1 × 107) were subcutaneously implanted into the right hind flanks of 5-6-week-old male nude mice[1]
Dosage: 15 mg/kg
Administration: i.p., once every two days, 23 days
Result: Achieved tumor growth inhibition (TGI) rate of 34.1% in A549 xenograft mice and a higher tumor growth inhibition (TGI) rate of 65.8% in A549/Taxol (Taxol-resistant) xenograft mice.
Showed no significant changes in body weight.
分子量

657.67

Formula

C35H35N3O10
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

PROTAC tubulin-Degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

PROTAC tubulin-Degrader-1PROTACsMicrotubule/TubulinApoptosisnon-small cell lung cancer (NSCLC)PROTAC,α/β/β3-tubulinA549/Taxol cellsInhibitorinhibitorinhibit

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