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6-diaMine

(CAS No:937263-43-9)
ARRY-380 (ONT-380) is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity.
CAS No:937263-43-9
Molecular Weight(MW):480.52
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 937263-43-9
Molecular formula(MF) C26H24N8O2
Molecular Weight(MW): 480.52
Alias
Solubility
In vitro DMSO 96 mg/mL (199.78 mM)
Ethanol 15 mg/mL (31.21 mM)
Water <1 mg/mL
In vivo
Biological Activity
Description ARRY-380 (ONT-380) is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity.
Targets
p95 HER2 [2] ErbB2 [2] EGFR [2]
7 nM 8 nM 4000 nM
In vitro

The compound is a reversible, ATP-competitive inhibitor with nanomolar potency against ErbB2 in both in vitro and in cell-based assays[1]. In cell-based assays, ARRY-380 is ~500-fold selective for HER2 vs. EGFR and is equipotent against truncated p95-HER2[2].

In vivo In vivo, ARRY-380 significantly inhibits tumor growth in multiple HER2-dependent tumor xenograft models[2]. It shows excellent activity in numerous mouse tumor models including breast (BT-474, MDA-MB-453), ovarian (SKOV-3) and gastric (N87) carcinoma models. In the BT-474 model, ARRY-380 demonstrated significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size)[1].