1. Protein Tyrosine Kinase/RTK
  2. Ephrin Receptor
  3. LDN-211904

LDN-211904 是一种强效且可逆的 EphB3 抑制剂,IC50 为 79 nM。LDN-211904 在小鼠肝微粒体中表现出良好的代谢稳定性。LDN-211904 与 Cetuximab (HY-P9905) 联合使用可有效抑制 STAT3 激活的结肠直肠癌 (CRC) 干细胞和 CRC 中的西妥昔单抗耐药性。

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LDN-211904

LDN-211904 Chemical Structure

CAS No. : 1198408-39-7

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MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

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生物活性

LDN-211904 is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 shows good metabolic stability in mouse liver microsomes. LDN-211904 with cetuximab could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab (HY-P9905) resistance in CRC[1][2].

体外研究
(In Vitro)

LDN-211904 (20 μM; 24 h) 通过增加 SW48 抗性细胞中的 c-PARP 来诱导细胞凋亡[2]
LDN-211904 (20 μM; 4-20 h) 降低 SW48 抗性细胞中的 p-STAT3、GLI-1、SOX2 和波形蛋白的水平[2]

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

Apoptosis Analysis[2]

Cell Line: SW48 and SW48 Cetuximab-resistant (SW48R) cells
Concentration: 20 μM
Incubation Time: 24 h
Result: Induced apoptosis by increasing c-PARP.

Western Blot Analysis[2]

Cell Line: SW48 and SW48 Cetuximab-resistant (SW48R) cells
Concentration: 20 μM
Incubation Time: 4 h, 8 h, 20 h
Result: The levels of p-STAT3, GLI-1, SOX2 and Vimentin in SW48 resistant cells were decreased.
体内研究
(In Vivo)

LDN-211904(0.1 mg/kg;腹腔注射;每周三次;持续 21 天)可抑制并克服体内 Cetuximab (HY-P9905) 耐药性[2]

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

Animal Model: Four-week-old female BALB/c nude mice were implanted subcutaneously SW48 cells[2]
Dosage: 0.1 mg/kg
Administration: i.p.; three times a week; for 21 days
Result: Inhibited tumor growth.
分子量

354.83

Formula

C19H19ClN4O

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
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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.

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产品名称:
LDN-211904
目录号:
HY-136358
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