SYR127063
SYR127063 is a potent and selective human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitor with an IC50 of 11 nM. SYR127063 binds to the active site of the HER2 kinase domain in an ATP-competitive manner, thereby preventing the formation of the conserved salt bridge required for kinase activation. SYR127063 can be used in research related to breast cancer, ovarian cancer and gastric cancer.
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- CAS No.: 871026-18-5
- Formule: C23H20ClF3N4O3
- Masse moléculaire:492.88
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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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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
HER2 11 nM (IC50) |
HER4 >10000 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| BT-474 | GI50 |
27 nM
Compound: 12j
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Growth inhibition of human BT474 cells overexpressing HER2 gene after 5 days by particle analyzer
Growth inhibition of human BT474 cells overexpressing HER2 gene after 5 days by particle analyzer
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[PMID: 22003817] |
In Vitro
SYR127063 (preincubated for 5 min followed by a 10 min reaction with ATP) potently and selectively inhibits purified human HER2 kinase, with an IC50 of 11 nM. Its activity against human EGFR is approximately 40-fold weaker, and it shows no significant activity against human HER4[1].
SYR127063 (1 mM; incubated on ice for 1 h before use for crystallization, used to observe the resting state) binds to the ATP pocket and stabilizes a specific conformation of HER2 in a cell-free system[1].
SYR127063 binds tightly to the intracellular kinase domain (HER2in) of human HER2, with an average binding affinity of -11.0 kcal/mol, and forms stable interactions with the binding site in subdomain II of this receptor[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 871026-18-5
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Masse moléculaire 492.88
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Formule C23H20ClF3N4O3
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SMILES
FC(F)(F)C=1C=CC=C(OC2=CC=C(C=C2Cl)NC3=NC=NC=4C=CN(C43)CCOCCO)C1
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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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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)
SYR127063 Related Classifications
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