2. PROTAC JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  3. PROTACs EGFR Apoptosis Akt ERK
  4. PROTAC HER2 degrader-1

PROTAC HER2 degrader-1 是一种高的选择性 (IC50 =48.65 nM) 的 HER2 PROTAC 类降解剂，DC50 为 69 nM，Dmax 为 96%。PROTAC HER2 degrader-1 通过持久的 HER2 降解和对下游通路 (AKT 和ERK) 的强力抑制，抑制HER2阳性细胞增殖和肿瘤生长。PROTAC HER2 degrader-1 可用于 HER2 阳性癌症的研究。(粉色：HER2 配体：(HY-177009)；黑色：连接子；蓝色：CRBN 配体：(HY-W023573)。

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PROTAC HER2 degrader-1 Chemical Structure

PROTAC HER2 degrader-1 Chemical Structure

CAS No. : 2897640-93-4

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PROTAC HER2 degrader-1 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC HER2 degrader-1 is a and highly selective HER2 PROTAC degrader (IC50 = 48.65 nM), with a DC50 of 69 nM and a Dmax of 96%. PROTAC HER2 degrader-1 inhibits HER2-positive cell proliferation and tumor growth through persistent HER2 degradation and potent inhibition of downstream pathways (AKT and ERK). PROTAC HER2 degrader-1 can be used for research of HER2-positive cancers. (Pink: HER2 ligand: (HY-177009); Black: Linker; Blue: CRBN ligand: (HY-W023573)[1].

IC50 & Target[1]

HER2

69 nM (DC50)

CRBN-DDB1

 

体外研究
(In Vitro)

PROTAC HER2 degrader-1 (Compound CH7C4) (0.1-3 μM，24 小时) 可降解 BT-474 细胞中的 HER2，优于 A431 细胞中的 EGFR[1]。

PROTAC HER2 degrader-1 (0-10 μM，72 小时) 在 A431 细胞中浓度高达 10 μM 时，对 A431 细胞增殖无抑制作用[1]。

PROTAC HER2 degrader-1 可抑制 HER2 驱动的乳腺癌细胞系 BT-474 和 SK-BR-3 以及胃癌细胞系 NCI-N87 的增殖，IC50 值分别为 0.047 nM、0.098 nM 和 0.137 nM[1]。

PROTAC HER2 degrader-1 (0-100 nM) 可诱导 BT-474 细胞凋亡，并抑制 BT-474 细胞周期的 G1 期[1]。

PROTAC HER2 degrader-1 (0-1 μM) 以浓度依赖性方式在 BT-474 (DC50 = 69 nM，Dmax = 96%) 和 NCI-N87 细胞 (DC50 = 55 nM，Dmax = 94%) 中诱导 HER2 高效降解[1]。

PROTAC HER2 degrader-1 (200 nM，0-24 小时) 诱导 BT-474 细胞和 NCI-N87 细胞中HER2 降解并抑制 AKT 和 ERK 磷酸化[1]。

PROTAC HER2 degrader-1 (200 nM，24 小时) 通过泛素蛋白酶体系统 (UPS) 诱导 BT-474 细胞中泛素化介导的 HER2 降解[1]。

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

PROTAC HER2 degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: A431 cells
Concentration: 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time: 24 h
Result: Induced almost complete degradation of HER2, and a significant hook effect was observed at 3 μM, without significantly affecting EGFR levels in A431 cells.

Apoptosis Analysis[1]

Cell Line: BT-474 cells
Concentration: 0 nM, 10 nM, 50 nM, 100 nM
Incubation Time:
Result: Induced apoptosis (63% at 50 nM) and inhibited G1 cell cycle (84% at 100 nM) in BT-474 cells.

Western Blot Analysis[1]

Cell Line: BT-474 cells, NCI-N87 cells
Concentration: 10 nM, 100 nM, 250 nM, 1000 nM
Incubation Time: 24 h
Result: Induced HER2 degradation and blocked signal transduction in a concentration-dependent manner.
Reduced HER2 autophosphorylation.
Inhibited phosphorylation of key HER2 oncogenic-associated kinases AKT and ERK without affecting their protein levels.

Western Blot Analysis[1]

Cell Line: BT-474 cells, NCI–N87 cells
Concentration: 200 nM
Incubation Time: 0 h, 3 h, 6 h, 12 h, 24 h
Result: Induced significant degradation of HER2 within 3 h.
Induced almost complete degradation of HER2 at 24 h and significantly inhibited AKT and ERK phosphorylation.

Western Blot Analysis[1]

Cell Line: BT-474 cells
Concentration: 200 nM
Incubation Time: 24 h
Result: Degraded HER2, this degradation was completely inhibited after pretreatment with MLN4924 (HY-70062), MG132 (HY-13259), lenalidomide (HY-A0003), and Tucatinib (HY-16069).
体内研究
(In Vivo)

PROTAC HER2 degrader-1 (Compound CH7C4) ( 5 mg/kg，10 mg/kg，静脉注射，每天一次，21 天) 可抑制携带 BT-474 异种移植肿瘤的 BALB/c 裸鼠的肿瘤生长[1]。

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

Animal Model: BALB/c nude mice bearing BT-474 (i.p., 1 × 107) xenograft tumors[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: i.v., once a day, 21days
Result: Showed weaker antitumor activity than 10 mg/kg Tucatinib at a dose of 5 mg/kg, with TGI values of 47% and 64%, respectively
Showed superior antitumor activity compared with Tucatinib at a dose of 10 mg/kg (TGI: 73% vs. 64%).
Degraded HER2, and no significant side effects or weight loss were observed during treatment.
分子量

910.03

Formula

C49H55N11O7
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

PROTAC HER2 degrader-1 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:

PROTAC HER2 degrader-12897640-93-4PROTACsEGFRApoptosisAktERKEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BExtracellular signal regulated kinasesDegraderA431 cellsBT-474 cellsSK-BR-3 cellsNCI-N87 cellsBALB/c nude miceBT-474 xenograft tumorsInhibitorinhibitorinhibit

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