中文名：OSI-420
英文名：OSI-420
英文別名：DesMethyl Erlotinib (CP-473420) HCl;2-(4-(3-ethynylphenylamino)-7-(2-methoxyethoxy)quinazolin-6-yloxy)ethanol hydrochloride
純度：10mM in DMSO
貨號(hào)：O408234
包裝：1ml
Cas號(hào)：183320-51-6
存儲(chǔ)溫度：-80℃儲(chǔ)存
產(chǎn)品介紹：
Information
OSI-420 (DesMethyl Erlotinib, CP-473420) is the active metabolite of Erlotinib (EGFRinhibitor withIC50of 2 nM).
In?vitro
OSI-420 is the major metabolite of Erlotinib in human plasma. Erlotinib disappearance from plasma after a short IV infusion is biexponential with a mean terminal half-life of 5.2 h and a mean clearance of 128 ml/min per m(2). OSI-420 exposure (AUC) in plasma is 30% (range 12-59%) of erlotinib, and OSI-420 clearance is more than 5-fold higher than erlotinib. Erlotinib and OSI-420 are equipotent, and the combined concentrations of erlotinib + OSI-420 achieved in the CSF exceeded the IC50 (7.9 ng/ml or 20 nM) for the EGFR tyrosine kinase inhibition in intact tumor cells. Erlotinib potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi human colon cancer cells andMDA MB-468 human breast cancer cells. Erlotinib (1 μM) induces apoptosis in DiFi human colon cancer cells. Erlotinib inhibits growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 μM. Erlotinib(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of Erlotinib inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. Combination with Erlotinib could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition.
In?vivo
At doses of 100 mg/kg, Erlotinib completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice. Erlotinib reduces the growth of xenografted human AML cells.
Cell?Data
cell?lines：
Concentrations：30 nM-20 μM
Incubation?Time：72 hour
Powder?Purity:≥99%
查看阿拉丁官網(wǎng)此產(chǎn)品相關(guān)對(duì)應(yīng)頁(yè)面：https://www.aladdin-e.com/zh_cn/O408234.html
關(guān)鍵字： DesMethyl Erlotinib (CP-473420) HCl;2-(4-(3-ethynylphenylamino)-7-(2-methoxyethoxy)quinazolin-6-yloxy)ethanol hydrochloride
上海阿拉丁生化科技股份有限公司是A股上市公司（（股票代碼：688179），專注于科研試劑的研發(fā)、生產(chǎn)和銷(xiāo)售，已陸續(xù)建立多個(gè)工廠和研發(fā)中心。作為領(lǐng)軍企業(yè)，阿拉丁始終堅(jiān)持質(zhì)量第一，連續(xù)13年被評(píng)為“最受歡迎試劑品牌”。
阿拉丁目前常備庫(kù)存試劑產(chǎn)品品種超過(guò)7萬(wàn)種，SKU總數(shù)超過(guò)46萬(wàn)，產(chǎn)品線涵蓋了化學(xué)試劑、生化試劑、藥靶配體、蛋白質(zhì)和抗體等多個(gè)領(lǐng)域，是國(guó)內(nèi)少數(shù)化學(xué)試劑到生物試劑全面發(fā)展的國(guó)產(chǎn)試劑品牌，產(chǎn)品同步發(fā)布在我們國(guó)內(nèi)外電商平臺(tái)。