Bpsbioscience/EPZ004777/27622/5 mg
商品编号：
27622
品牌：
bpsbioscience
市场价：
¥4100.00
美元价：
2460.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
MW: 539.7 Da
CAS Registry #: 1338466-77-5
Formula: C28H41N7O4
Target: Dot1L
Background:
EPZ004777 selectively inhibits cellular H3K79 methylation and inhibits expression of key MLL fusion target genes. EPZ004777 produces potent antitumor efficacy, and significantly increases median survival in a mouse xenograft model of MLL leukemia. Following DOT1L inhibition, EPZ004777 selectively inhibits proliferation of MLL-rearranged cell lines and MLL-AF9-transformed murine hematopoietic cells. In addition, EPZ004777 also induces differentiation and apoptosis in MLL-rearranged cells. DOT1L inhibition by EPZ004777 results in significantly decreased proliferation, decreased expression of MLL-AF6 target genes, and cell cycle arrest of MLL-AF6-transformed cells. 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.
Description:
EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 400 pM. EPZ004777 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.
Synonym(s):
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
Biological Activity:
EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 400 pM. EPZ004777 also exhibits anti-proliferative activity against both MLL-rearranged and non-rearranged human leukemia cell lines, including RS4;11 (IC50: 6.47 µM), SEM (IC50: 1.72 µM), MV4-11 (IC50: 0.17 µM), THP-1 (IC50: 3.36 µM), MOLM-13 (IC50: 0.72 µM), KOPN-8 (IC50: 0.62 µM), REH (IC50: 13.9 µM), Kasumi-1 (IC50: 32.99 µM) and 697 (IC50: 36.57 µM)
Solubility:
Soluble in DMSO
Storage / Stability:
Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Reference(s):
1. Yu W, Cet al. Nat Commun. 2012;3:1288.
2. Chen L,et al. 2013 Apr;27(4):813-22.
2. Chen L,et al. 2013 Apr;27(4):813-22.
Scientific Category:
Methyltransferase Inhibitor
Product Type:
Inhibitor
Data shown is lot-specific. Contact us for specific information on other lots.
品牌介绍
bpsbioscience简介：为生命科学研究提供ELISA试剂盒（仅供科研）、抗体和抗原（仅供科研）、流式抗体，使您的检测结果更稳定可靠，用心服务科研。我公司国内总代理,华东地区代理bpsbioscience 专业经营进口胎牛血清、细胞因子、ELISA试剂盒、细胞、抗体、生物试剂、耗材、培养基、一抗、二抗、其产品吸附均匀，吸附性好，空白值低，孔底透明度高，代做ELISA实验等。
