This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
EGFR/HER2-IN-6
Catalog No. T61732
EGFR/HER2-IN-6 (compound 43) is a dual EGFR/HER2 and DHFR inhibitor with potent activity against EGFR kinase, HER2 kinase, and DHFR, characterized by IC50 values of 0.122 μM, 0.078 μM, and 0.585 μM, respectively. This compound displays notable anticancer properties in various cancer cell lines, while demonstrating a favorable safety profile and selectivity indices. Consequently, EGFR/HER2-IN-6 holds promise as a valuable tool in cancer research [1].
All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
EGFR/HER2-IN-6 (compound 43) is a dual EGFR/HER2 and DHFR inhibitor with potent activity against EGFR kinase, HER2 kinase, and DHFR, characterized by IC50 values of 0.122 μM, 0.078 μM, and 0.585 μM, respectively. This compound displays notable anticancer properties in various cancer cell lines, while demonstrating a favorable safety profile and selectivity indices. Consequently, EGFR/HER2-IN-6 holds promise as a valuable tool in cancer research [1].
In vitro
EGFR/HER2-IN-6 demonstrates a notable broad-spectrum cytotoxicity across various cell lines, including HepG2 hepatocellular carcinoma, MCF7 breast cancer, HCT-116 colorectal carcinoma, PC-3 prostate, and HeLa cervical epithelioid carcinoma, as well as lower toxicity toward WI-38 normal fetal lung fibroblasts. Particularly against MCF7 cells, its cytotoxic effects are superior to those of SOR, with IC50 values ranging from 2.37 to 18.39 μM for cancer cells and 36.84 μM for normal cells after 72 hours exposure to concentrations up to 100 μM. Additionally, at lower concentrations (0-20 μM) and shorter exposure times (0-48 hours), EGFR/HER2-IN-6 disrupts the cell cycle and triggers apoptosis, specifically in MCF-7 breast cancer cells, favoring anti-cancer activity through mechanisms that include cell cycle arrest at the G1/S and G1 phases rather than inducing necrosis.
In vivo
EGFR/HER2-IN-6, administered intraperitoneally at a dosage of 10 mg/kg once daily for 20 days, exhibits significant anti-breast cancer activity in 8-week-old Swiss albino female mice. The treatment resulted in a 65.3% decrease in tumor volume and a 7.4% reduction in body weight after 20 days, demonstrating its potential efficacy in combating breast cancer (1).
Molecular Weight
387.46
Formula
C18H21N5O3S
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dose Conversion
You can also refer to dose conversion for different animals.
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Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.