
簡(jiǎn)要描述:Irbinitinib 937263-43-9Irbinitinib(ARRY-380; ONT-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.
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| 品牌 | absin | CAS | 937263-43-9 |
|---|---|---|---|
| 分子式 | C26H24N8O2 | 純度 | 98% |
| 分子量 | 480.52 | 貨號(hào) | abs47028012 |
| 規(guī)格 | 10mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a potent and selective HER2 inhibitor | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
Irbinitinib 937263-43-9
| 產(chǎn)品描述 | |
| 描述 | Irbinitinib(ARRY-380; ONT-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. |
| 純度 | 98% |
| 儲(chǔ)存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 可溶性/溶解性 | 10 mM in DMSO |
| 生物活性 | |
| 靶點(diǎn) | p95 HER2 ,ErbB2 |
| In vitro(體外研究) | 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(體內(nèi)研究) | 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). |
| 參考文獻(xiàn) | |
| 參考文獻(xiàn) |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | CancerTumor biomarkersOncoproteins CancerTumor immunologyTumor-associated antigens NeuroscienceDevelopment Signal TransductionProtein PhosphorylationTyrosine KinasesReceptor Tyrosine Kinases Tags & Cell MarkersCell Type MarkersTumor Associated Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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