中文名：ABT-737
英文名：ABT-737
英文別名：Benzamide, 4-[4-[(4'-chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]-
純度：10mM in DMSO
貨號：A408945
包裝：1ml
Cas號：852808-04-9
存儲溫度：-80℃儲存
產(chǎn)品介紹：
Information
ABT-737 is a BH3 mimetic inhibitor ofBcl-xL,Bcl-2andBcl-wwithEC50of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 inducesmitochondrial pathway apoptosisandmitophagy. Phase 2.
In?vitro
ABT-737 shows low activity to Bcl-B and no effects to Mcl-1 and BFL-1. ABT-737 is sensitive to HL60, KG1 and NB4 cells with IC50 of 50 nM, 80 nM and 80 nM, respectively. ABT-737 induces apoptosis in HL60 cells, which due to decreased Bcl-2/Bax heterodimerization and has no effect on cell cycle distribution. ABT-737 also induces cytochrome c release from purified mitochondria and promotes conformational changes in Bax that are associated with apoptosis. Resistant cells (Hela and MCF-7) can be sensitized to ABT-737 by approaches that down-regulate, destabilize, or inactivate Mcl-1. ABT-737 also causes Bax/BAK-dependent cytochrome c release only when Mcl-1 has been neutralized. ABT-737 displaces Bim from Bcl2\'s BH3-binding pocket, allowing Bim to activate Bax, induce mitochondrial permeabilization, and rapidly commit the primary chronic lymphocytic leukemia (CLL) cells to death. Knockdown of Mcl-1 with siRNA sensitizes two resistant SCLC cell lines H196 and DMS114 to ABT-737 by enhancing the induction of apoptosis. Likewise, up-regulation of Noxa sensitizes H196 cells to ABT-737. ABT-737 inhibits proliferation and induces apoptosis in many SCLC cell lines including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146 and etc. Bcl-2 and Noxa may contribute mechanistically to the cellular response to ABT-737 in NCI-H146 cells. A recent study shows that ABT-737 significantly induces apoptosis in HTLV-1 infected T-cell lines as well as in fresh ATLL cells.
In?vivo
In aggressive leukemia model, ABT-737 suppresses the leukemia burden by 53% at the 30 mg/kg, with significantly extended survival of mice. ABT-737 does not induce significantly abnormalities in blood cell counts or serum chemistries. ABT-737 prolongs the survival of recipient mice transplanted with Bcl-2-transduced tumors. ABT-737 shows great antitumor activity in an ATLL mouse model at a dose of 100 mg/kg.
Cell?Data
cell?lines：
Concentrations：0.001-10 μM
Incubation?Time：48 hours
Powder?Purity:≥97%
查看阿拉丁官網(wǎng)此產(chǎn)品相關(guān)對應頁面：https://www.aladdin-e.com/zh_cn/A408945.html
關(guān)鍵字： Benzamide, 4-[4-[(4'-chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]-
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)和銷售，已陸續(xù)建立多個工廠和研發(fā)中心。作為領(lǐng)軍企業(yè)，阿拉丁始終堅持質(zhì)量第一，連續(xù)13年被評為“最受歡迎試劑品牌”。
阿拉丁目前常備庫存試劑產(chǎn)品品種超過7萬種，SKU總數(shù)超過46萬，產(chǎn)品線涵蓋了化學試劑、生化試劑、藥靶配體、蛋白質(zhì)和抗體等多個領(lǐng)域，是國內(nèi)少數(shù)化學試劑到生物試劑全面發(fā)展的國產(chǎn)試劑品牌，產(chǎn)品同步發(fā)布在我們國內(nèi)（www.aladdin-e.com）和海外（www.aladdinsci.com）電商平臺。