2. Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. EGFR Apoptosis
  4. 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.

For research use only. We do not sell to patients.

HER2-IN-22 Chemical Structure

HER2-IN-22 Chemical Structure

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HER2-IN-22 Related Antibodies

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Description

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[1].

IC50 & Target[1]

HER2

215 μM (IC50)

In Vitro

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.

HER2-IN-22 Related Antibodies

Apoptosis Analysis[1]

Cell Line: BT474
Concentration: 0.5 μM, 1 μM, 5 μM, 10 μM
Incubation Time: 72 h
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 %.
In Vivo

HER2-IN-22 (compound 3f) (10 mg/kg; i.p.; single dose) exerts anti-tumor activity in in vivo breast cancer model[1].

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

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]
Dosage: 10 mg/kg
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
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.
Molecular Weight

576.24

Formula

C26H16Br2N4O2
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HER2-IN-22 Related Classifications

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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.

Keywords:

HER2-IN-22EGFRApoptosisEpidermal growth factor receptorErbB-1HER1PyrazolopyridinesAntitumorDockingMolecular dynamicsBreast cancerBT474Inhibitorinhibitorinhibit

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