產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
EPZ004777 | 10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg | 1338466-77-5 | EY-Y0165365 |
Cas No.1338466-77-5
別名 N/A
化學名 1-[3-[[(2R,3S,4R,5R)-5-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxyoxolan-2-yl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea
分子式 C28H41N7O4
分子量 539.67
溶解度 ≥ 27 mg/mL in DMSO, ≥ 94.6 mg/mL in EtOH with ultrasonic
儲存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
EPZ004777 is a specific small-molecule H3K79 methyltransferase DOT1L inhibitor that potently inhibits DOT1L in a radionuclide homogeneous assay with the half maximal inhibition concentration IC50 value of 400 pM and selectively kills a variety of MLL-rearranged leukemia cells, including an MLL-AF4 leukemia cell line MV4-11 and an MLL-AF9 leukemia cell line MOLM13 [1 & 2].
EPZ004777 has also been found to selectively inhibit the proliferation of MLL-AF10 and CALM-AF10 transformed cells in a dose dependent manner (IC50: 0.1 μM to 1 μM), in which the mRNA expression levels of two hallmark leukemogenic genes (Hoxa9 and Meis1) are suppressed by EPZ004777 in a concentration dependent manner [2].
Reference
References:
[1] Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304.
[2] Chen L, Deshpande AJ, Banka D, Bernt KM, Dias S, Buske C, Olhava EJ, Daigle SR, Richon VM, Pollock RM, Armstrong SA. Abrogation of MLL-AF10 and CALM-AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1l. Leukemia. 2013 Apr;27(4):813-22. doi: 10.1038/leu.2012.327. Epub 2012 Nov 9.
關(guān)鍵字： 1338466-77-5;C28H41N7O4;EPZ004777;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學、分子生物學和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè)，公司自成立以來，秉承""全心全意服務(wù)于科研工作者""的企業(yè)理念，立足生物科技領(lǐng)域，運用生物技術(shù)和科研試劑，發(fā)展現(xiàn)代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品，服務(wù)生物科技領(lǐng)域的科學研究人員。
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