2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs c-Met/HGFR Apoptosis
  4. PROTAC c-Met degrader-6

PROTAC c-Met degrader-6 是一种强效且口服有效的 c-Met PROTAC 降解剂。PROTAC c-Met degrader-6 显著诱导 c-Met 蛋白的降解，在 EBC-1 和 Hs746T 细胞中，其 DC50 值分别为 0.52 nM 和 0.45 nM。PROTAC c-Met degrader-6 几乎完全消除了肿瘤细胞的迁移和侵袭能力，显著诱导细胞凋亡 (apoptosis)，并阻断细胞周期于 G0/G1 期。PROTAC c-Met degrader-6 可用于多种癌症的研究，例如非小细胞肺癌和胃癌 (粉色: c-Met 配体 (HY-W425461); 蓝色: E3 连接酶配体 (HY-14658); 黑子: 连接子 (HY-20797); 靶蛋白配体 + 连接子 (HY-175337))。

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PROTAC c-Met degrader-6

PROTAC c-Met degrader-6 Chemical Structure

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PROTAC c-Met degrader-6 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 c-Met degrader-6 is a potent and orally active c-Met PROTACdegrader. PROTAC c-Met degrader-6 significantly induces the degradation of the c-Met protein with DC50s of 0.52 nM and 0.45 nM in EBC-1 and Hs746T. PROTAC c-Met degrader-6 almost abrogates the migratory and invasion abilities of tumor cells and significantly induces the apoptosis and blocks the cell cycle in the G0/G1 phase. PROTAC c-Met degrader-6 can be used for the study of various cancers such as non-small cell lung cancer and stomach cancer (Pink: c-Met ligand (HY-W425461); Blue: E3 ligand (HY-14658); Black: Linker (HY-20797))[1].

IC50 & Target[1]

c-Met

 

体外研究
(In Vitro)

PROTAC c-Met degrader-6 (Compound G4) (72 h) 具有抗增殖功效，在 EBC-1、Hs746T 和 MHCC97H 细胞中的 IC50 值分别为 3.55、3.01 和 7.48 nM[1]。
PROTAC c-Met degrader-6 (1-10 nM，48 h) 在 EBC-1 和 Hs746T 细胞中通过泛素-蛋白酶体途径显著降解 c-Met[1]。
PROTAC c-Met degrader-6 (5-10 nM，24-48 h) 在诱导细胞凋亡、G1 期细胞周期阻滞以及抑制细胞迁移和侵袭方面表现出强大的作用[1]。
PROTAC c-Met degrader-6 (100-1000 nM, 48 h-3 days) 对携带 c-MetD1228N 和 c-MetY1230H 突变体的 EBC-1 和 Hs746T 细胞具有优异的抗增殖作用[1]。
PROTAC c-Met degrader-6 在人肝微粒体和小鼠肝微粒体中具有良好的代谢稳定性[1]。

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

PROTAC c-Met degrader-6 相关抗体:

Apoptosis Analysis[1]

Cell Line: EBC-1 and Hs746T cells
Concentration: 10 nM
Incubation Time: 48 h
Result: Produced the apoptosis rates of 21.8% in EBC-1 and observed similar results in Hs746T.

Cell Cycle Analysis[1]

Cell Line: EBC-1 and Hs746T cells
Concentration: 10 nM
Incubation Time: 48 h
Result: Induced cell cycle arrest at the G0/G1 phase.

Cell Migration Assay [1]

Cell Line: EBC-1 and Hs746T cells
Concentration: 5 nM
Incubation Time: 24 h
Result: Significantly inhibited the migratory capacity.

Cell Invasion Assay[1]

Cell Line: EBC-1 and Hs746T cells
Concentration: 5 nM
Incubation Time: 24 h
Result: Significantly inhibited the invasive capacity.

Western Blot Analysis[1]

Cell Line: EBC-1 and Hs746T cells
Concentration: 1 and 10 nM
Incubation Time: 48 h
Result: Significantly inhibited the levels of c-Met phosphorylation (p-c-Met) and STAT3 phosphorylation (p-STAT3) at 1nM
Completely blocked the c-Met degradation effect pretreatment with MLN4924 (E1 ubiquitin-activating enzyme inhibitor) (HY-70062) and MG132 (proteasome inhibitor) (HY-13259).

Western Blot Analysis[1]

Cell Line: EBC-1 and Hs746T cells harboring a D1228N mutation
Concentration: 100 and 1000 nM
Incubation Time: 48 h
Result: Inhibited the p-c-Met level, and complete c-Met degradation and p-c-Met inhibition.
体内研究
(In Vivo)

PROTAC c-Met degrader-6 (Compound G4) (5-10 mg/kg, p.o., 每日一次共 18 天) 在 EBC-1 异种移植小鼠模型中能显著抑制肿瘤生长[1]。

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

Animal Model: EBC-1 xenografts model established in NOD/SCID mice (6 week-old)[1]
Dosage: 5 and 10 mg/kg
Administration: Orally administration (p.o.), once daily for 18 days
Result: Significantly inhibited EBC-1 tumor growth, with tumor growth inhibition (TGI %) values of 84.12% at 5 mg/kg and 99.28% at 10 mg/kg after 10 days
Demonstrated complete tumor inhibition during the extended period (by day 18) at 10 mg/kg.
Exhibited a notable reduction in the percentage of Ki67-and CD31-positive tumor cells and an Increased percentage of cleaved caspase 3-positive tumor cells.
Exhibited more potent effects on reducing the level of p-c-Met and p-STAT3.
No obvious body weight loss and no other obvious toxic signs.
分子量

749.77

Formula

C41H35N9O6
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 c-Met degrader-6 相关分类

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  • 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:

PROTAC c-Met degrader-6PROTACsc-Met/HGFRApoptosisEBC-1 cellsHs746T cellsMHCC97H cellsXenograft mice modelPROTACInhibitorinhibitorinhibit

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