1. Membrane Transporter/Ion Channel Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  2. GLUT EGFR Apoptosis
  3. GLUT1/EGFR-IN-1

GLUT1/EGFR-IN-1 (compound H) 是 GLUT1EGFR 的强效抑制剂。GLUT1/EGFR-IN-1 可同时作用于 EGFR 酪氨酸激酶 ATP 结合位点并抑制 GLUT1 介导的能量代谢,导致 ATP、MMP、细胞内乳酸和 EGFR 核转移减少。GLUT1/EGFR-IN-1 可用于鼻咽癌 (NPC) 和三阴性乳腺癌 (TNBC) 研究。

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GLUT1/EGFR-IN-1 Chemical Structure

GLUT1/EGFR-IN-1 Chemical Structure

CAS No. : 2393787-80-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of GLUT1 and EGFR. GLUT1/EGFR-IN-1 can simultaneously act on the EGFR tyrosine kinase ATP-binding site and inhibit GLUT1-mediated energy metabolism, resulting in reductions in ATP, MMP, intra-cellular lactic acid, and EGFR nuclear transfer. GLUT1/EGFR-IN-1 can be used for nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC) research[1].

IC50 & Target

GLUT1

 

EGFR

 

体外研究
(In Vitro)

GLUT1/EGFR-IN-1 (compound H) 在 CNE1 和 MDA-MB231 细胞中表现出优异的抗肿瘤活性,IC50 值低于 3 µmol/L,但在 CNE2 细胞中活性不明显[1]
GLUT1/EGFR-IN-1 (0-4 μM,48 小时)抑制 CNE1 和 MDA-MB231 细胞中 EGFR 和 p-EGFR 的表达[1]
GLUT1/EGFR-IN-1 (0-4 μM,48 小时)诱导 CNE1 和 MDA-MB231 细胞凋亡[1]

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

Western Blot Analysis[1]

Cell Line: CNE1 and MDA-MB231 cells
Concentration: 1 μmol/L, 2, 4 μmol/L
Incubation Time: 48 h
Result: Depressed the expression of EGFR-, p-EGFR- and GLUT1-mediated glycolysis-related proteins.
体内研究
(In Vivo)

GLUT1/EGFR-IN-1 (compound H) (4-8 mg/kg,腹腔注射,2周)抑制裸鼠模型中 MDA-MB231 移植肿瘤细胞的生长[1]

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

Animal Model: BALB/c-neu female mice (Four- to five-week-old, n=5)[1]
Dosage: 4, 8 mg/kg
Administration: IP, for two weeks
Result: Inhibited the growth of the MDA-MB231 transplanted tumour model in nude mice.
分子量

696.75

Formula

C44H32N4O5

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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  • 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.

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产品名称:
GLUT1/EGFR-IN-1
目录号:
HY-163726
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