Tucatinib (Irbinitinib, ONT-380, ARRY-380) 是一种具有口服活性、可逆的、ATP竞争性的的ErbB2（HER2）小分子抑制剂。在细胞实验中，ARRY-380对ErbB-2和p95 HER2的IC50s分别为8 nM和7 nM，对HER2的选择性是对EGFR的500倍。具有潜在的抗肿瘤活性。 Information Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an oral, potent, selective, reversible and ATP-competitive small-molecule inhibitor ofErbB-2(also called HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively in cell-based assays, showing ~500-fold selective for HER2 vs EGFR. It has potential antineoplastic activity. Targets p95 HER2 (Cell-based assay); ErbB2 (Cell-based assay) 7 nM; 8 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. Incell-based assays, ARRY-380 is ~500-fold selective for HER2 vs. EGFR and is equipotent against truncated p95-HER2. In vivo ARRY-380 significantly inhibits tumor growth in multiple HER2-dependent tumor xenograft models. 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).
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
Tucatinib (Irbinitinib, ONT-380)
Dangerous GoodsCAS number：937263-43-9 molecular formula：C26H24N8O2
overview
compound introduction
Specs
| Chinese alias | 图卡替尼(厄比尼替尼，ONT-380) | ||
| English alias | Irbinitinib | ONT-380 | Q25100690 | 6-N-(4,4-dimethyl-5H-1,3-oxazol-2-yl)-4-N-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]quinazoline-4,6-diamine | UNII-234248D0HH | BDBM471617 | D11141 | Example 11 (WO2007059257A2) | N6-(4,5-Dihydro-4,4-dim | ||
| CAS number | 937263-43-9 | molecular formula | C26H24N8O2 |
| molecular weight | 480.52 g/mol | Exact mass | - |
| PSA | 111.000 Ų | logp | 4.744 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
