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HER2-Inhibitor-1 European Partner

Item no. S2752-50
Manufacturer Selleckchem
CASRN 937265-83-3
Amount 50 mg
Quantity options 10 mg 1 g 10 g 200 mg 5 mg 50 mg 5 g
Category
Type Inhibitors
Specific against other
Smiles CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)C4=CC=C(O4)CNCCS(=O)(=O)C)OC5=CC6=NC=NN6C=C5
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias HER2,HER2
Similar products Arry-380
Available
Storage Conditions
2 years -80 in solvent
Molecular Weight
569, 63
Clinical Trials
ARRY-380 is in a phase I clinical trial for the treatment of breast cancer.
IC50
8 nM [1], 8 nM [1], 8 nM [1], 8 nM [1], 8 nM [1], 8 nM [1]
In vitro
ARRY-380 is equipotent against truncated p95-HER2 with IC50 of 7 nM. [1] However, ARRY-380 suppresses EGFR with IC50 of 4 uM. ARRY-380 is about 500-fold selective for HER2 versus EGFR. [1]
In vivo
ARRY-380 significantly prevents the growth of tumor in multiple HER2-dependent tumor xenograft models and displays additive activity in combination with standard-of-care agents. [1]
Solubility (25C)
DMSO 114 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information
HER2-Inhibitor-1 is an analog of ARRY-380. ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.
Chemical Name
N-(4-([1, 2, 4]triazolo[1, 5-a]pyridin-7-yloxy)-3-methylphenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-amine

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 50 mg
Available: In stock
available

Delivery expected until 9/25/2025 

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