HER2-IN-23
HER2-IN-23 is a selective HER2 inhibitor. HER2-IN-23 reduces in total HER2 expression rather than in phosphorylated HER2 (p-HER2). HER2-IN-23 reduces cyclin D1 level and stimulates PARP cleavage. HER2-IN-23 can be used for the study of HER2-positive breast cancer.
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- Formule: C22H16ClFO4
- Masse moléculaire:398.81
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
In Vitro
HER2-IN-23 (Compound 4o) (0.4-25 μM, 72 h) shows moderate antiproliferative activity against HER2-positive cells (such as BT474 (IC50 = 10.5 μM), A431 (IC50 = 9.9 μM), and HCC1954 (IC50 = 8.5 μM)), but exhibits lower activity against HER2-negative cells (such as MDA-MB-231 (IC50 = 19.7 μM) and MCF7 (IC50 = 12.8 μM))[1].
HER2-IN-23 (1 μM) inhibits HER2 kinase by 84% at a concentration of 1 μM, while showing low or no inhibition against other kinases (such as EGFR, HER4, IGF1R, etc.)[1].
HER2-IN-23 (10 μM, 24 h) significantly reduces total HER2 expression in A431 cells, but phosphorylated HER2 (p-HER2) shows no significant change; simultaneously, cyclin D1 expression is almost completely inhibited, and an increase in PARP cleavage is observed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:A431 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Significantly reduced total HER2 expression in A431 cells, but phosphorylated HER2 (p-HER2) showed no significant change; simultaneously, cyclin D1 expression was almost completely inhibited, and an increase in PARP cleavage was observed.
Chemical Information
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Masse moléculaire 398.81
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Formule C22H16ClFO4
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SMILES
O=C1C(C2=CC=C(OCC3=CC=CC(F)=C3)C(Cl)=C2)=COC4=C1C(CCC4)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HER2-IN-23 Related Classifications
HY-178116 Related Classifications
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