HER2-IN-22
HER2-IN-22 is a potent and selective HER2 inhibitor with an IC50 of 215 μM. HER2-IN-22 possesses killing activity against various tumor cells and can induce cell apoptosis. HER2-IN-22 significantly inhibits tumor growth. HER2-IN-22 can be used in the study for tumors such as HER2+ breast cancer.
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- Fòrmula: C26H16Br2N4O2
- Peso molecular:576.24
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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HER2 215 μM (IC50) |
HER2-IN-22 (compound 3f) exhibits mean GI50 values of 1.9, 2.5, and 2.3 μM against leukemia, central nervous system, and breast cancer cell lines, respectively, in the NCI-60 cell line panel[1].
HER2-IN-22 (10 μM, 30 min) inhibits HER2 with an inhibition percentage of 88%[1].
HER2-IN-22 (0-50 μM, 72 h) demonstrates high antiproliferative activity against BT474, BT549 and ZR-75-30 with IC50 values of 323.3, 282.6 and 271.7 nM, respectively[1].
HER2-IN-22(0.5-10 μM, 72 h) induces the highest necrotic level at 10 μM of 10.5 % in BT474 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT474
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Concentration:0.5 μM, 1 μM, 5 μM, 10 μM
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Incubation Time:72 h
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Result:Induced a negligible level of early (4.7%) and late apoptosis (3%) at 5 μM.
Induced the highest necrotic level at 10 μM of 10.5 %.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Xenograft mouse model by 6-week-old female nude mice injected with 100 μL of ZR-75-30-luciferase 2×106 cells[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; after 1 and 7 weeks using the In Vivo Imaging System; tumor volume was measured twice a week for 7 weeks; histopathological analysis by the end of week 7
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Result:Had lower bioluminescence intensities.
Showed a significant inhibition in tumor size by 19.45%.
Reduced the tumor weight (p = 0.041) at the end of the experiment.
Chemical Information
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Peso molecular 576.24
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Fòrmula C26H16Br2N4O2
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SMILES
N#CC1=C(C2=CC=C(Br)C=C2)N=C(NN=C3C4=CC=C(Br)C=C4)C3=C1C5=CC=C(OC)C(O)=C5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HER2-IN-22 Related Classifications
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