2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Anaplastic lymphoma kinase (ALK)
  4. TD-004

TD-004 是一种强效的 ALK PROTAC 降解剂。TD-004 具有抗 ALK 抑制活性，其 IC50 为 0.11 µM，并能选择性抑制 SU-DHL-1 和 H3122 细胞 (ALK 阳性癌细胞) 的增殖，其 IC50 分别为 0.058 µM 和 0.28 µM。TD-004 通过招募 VHL E3 连接酶并利用蛋白酶体途径来诱导 ALK 融合蛋白的降解。在体内，TD-004 表现出显著的肿瘤生长抑制作用和良好的安全性。TD-004 可用于间变性大细胞淋巴瘤和非小细胞肺癌的研究。
(粉色: Anaplastic lymphoma kinase (ALK) 配体 (HY-15656)；蓝色: VHL 配体 (HY-125845)；黑色: 连接子)。

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TD-004

TD-004 Chemical Structure

CAS No. : 2162120-55-8

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TD-004 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

TD-004 is a potent ALK PROTAC degrader. TD-004 exhibits anti-ALK inhibitory activity with an IC50 of 0.11 µM and selectively inhibits the proliferation of SU-DHL-1 and H3122 cells (ALK-positive cancer cells) with IC50s of 0.058 µM and 0.28 µM, respectively. TD-004 induces degradation of ALK fusion proteins (NPM-ALK and EML4-ALK) via recruitment of the VHL E3 ligase and the proteasome pathway. TD-004 demonstrates significant tumor growth inhibition with a favorable safety profile in vivo. TD-004 can be used for the research of anaplastic large cell lymphoma and non-small cell lung cancer[1][2]. (Pink: Anaplastic lymphoma kinase (ALK) ligand (HY-15656); Blue: VHL ligand (HY-125845); Black: linker).

IC50 & Target[1]

VHL

 

体外研究
(In Vitro)

TD-004 具有抗 ALK 活性，其 IC50 为 0.11 µM，并能以微摩尔亲和力与 VHL 结合[1]。
TD-004 (1 µM) 在 SU-DHL-1 细胞中可降解 93% 的 NPM-ALK 蛋白，且此降解效力与其 ALK 抑制活性无关[1]。
TD-004 (0.03-30 µM, 8-16 小时) 在 NCI-H3122 细胞系中以时间和剂量依赖性的方式降解 EML4-ALK 融合蛋白[1]。
TD-004 (0.2-3 µM, 1-16 小时) 在 H3122 细胞中通过 E3 连接酶 VHL、在 SU-DHL-1 细胞中通过蛋白酶体介导的机制，有效诱导细胞内融合 ALK 蛋白的降解[1]。
TD-004 (3 天) 能选择性抑制 SU-DHL-1 和 H3122 癌细胞 (ALK 阳性细胞系) 的增殖，IC50 分别为 0.058 µM 和 0.28 µM，但不抑制 A549 细胞 (IC50 > 10 μM)[1]。

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

TD-004 相关抗体:

Western Blot Analysis[1]

Cell Line: NCI-H3122 cell
Concentration: 0.03, 0.3, 3 and 30 μM
Incubation Time: 8 or 16 h
Result: Degraded fusion protein EML4-ALK in dose-dependent manner for 16 h.
Slightly reduced ALK level at 8h treatment at high concentration, which indicated a time-dependent degradation pattern.

Western Blot Analysis[1]

Cell Line: H3122 cells
Concentration: 0.3 and 3 μM
Incubation Time: 1 h
Result: Induced ALK degradation, which was blocked by co-treatment with Epoxomicin (HY-13821) (1 μM).

Western Blot Analysis[1]

Cell Line: SU-DHL-1 cells
Concentration: 0.2 μM
Incubation Time: 16 h
Result: Mediated degradation of the NPM-ALK protein, which was inhibited by the VHL ligand.
体内研究
(In Vivo)

TD-004 (58 mg/kg，腹腔注射，每日一次，持续 14 天) 能在 H3122 移植瘤小鼠模型中有效抑制携带 ALK 融合蛋白的肿瘤的生长[1]。

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

Animal Model: H3122 cells (ALK-positive cells) (5 x 10 6) induced-female BALB/c nude mice[1].
Dosage: 58 mg/kg
Administration: i.p., once daily for 14 days
Result: Reduced tumor volume.
Did Not affect body weight.
分子量

1084.78

Formula

C55H70ClN9O8S2
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

TD-004 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

TD-0042162120-55-8TD004TD 004PROTACsAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246SU-DHL-1 cellsH3122 cellsanaplastic large cell lymphoma and non-small cell lung cancerInhibitorinhibitorinhibit

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