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HER2-IN-23 is a selective inhibitor of HER2 that reduces total HER2 expression instead of phosphorylated HER2 (p-HER2) levels. It lowers cyclin D1 levels and promotes PARP cleavage. HER2-IN-23 can be utilized in research on HER2-positive breast cancer.
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | HER2-IN-23 is a selective inhibitor of HER2 that reduces total HER2 expression instead of phosphorylated HER2 (p-HER2) levels. It lowers cyclin D1 levels and promotes PARP cleavage. HER2-IN-23 can be utilized in research on HER2-positive breast cancer. |
| In vitro | HER2-IN-23 (Compound 4o) exhibits moderate antiproliferative activity against HER2-positive cells, including BT474 (IC50 = 10.5 μM), A431 (IC50 = 9.9 μM), and HCC1954 (IC50 = 8.5 μM), within the concentration range of 0.4-25 μM over 72 hours. However, it shows lower activity against HER2-negative cells like MDA-MB-231 (IC50 = 19.7 μM) and MCF7 (IC50 = 12.8 μM). At a concentration of 1 μM, HER2-IN-23 inhibits the HER2 kinase by 84%, while its effect on other kinases, including EGFR, HER4, and IGF1R, is minimal or non-existent. Furthermore, treatment with HER2-IN-23 at 10 μM for 24 hours significantly reduces total HER2 expression in A431 cells without notably altering phosphorylated HER2 (p-HER2). Cyclin D1 expression is almost completely suppressed, and an increase in PARP cleavage is observed. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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