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Cat. No.: HY-111250

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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.

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

CAS No.: 871026-18-5
Formula: C₂₃H₂₀ClF₃N₄O₃
Molecular Weight:492.88

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

SYR127063 Chemical Structure

CAS No.: 871026-18-5

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One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target^[1]

HER2

11 nM (IC₅₀)

HER4

>10000 nM (IC₅₀)

All EGFR Isoforms :

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.

Chemical Information

CAS No. 871026-18-5
Molecular Weight 492.88
Formula C₂₃H₂₀ClF₃N₄O₃
SMILES

FC(F)(F)C=1C=CC=C(OC2=CC=C(C=C2Cl)NC3=NC=NC=4C=CN(C43)CCOCCO)C1
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

Handling Instructions (2659 KB)

References

[1]. Aertgeerts K, et al. Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein. The Journal of biological chemistry. 2011 May 27;286(21):18756-65.

[2]. Hakaman, H., et al. In-Silico molecular docking analysis of monoclonal antibodies, approved inhibitors, and plant-based inhibitors targeting extracellular and intracellular HER2 receptor. Berkala Penelitian Hayati, 31(1), 33–48.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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SYR127063

All EGFR Isoforms