| Company Name: |
Jinan Trio PharmaTech Co., Ltd.
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| Tel: |
+86 (531) 88811783 |
| Email: |
sales@trio-pharmatech.com (International market) |
| Products Intro: |
Product Name:EPZ004777 HCl
CAS:1380316-03-9
Purity:99% Package:5Mg, 10Mg, 20Mg, 50Mg
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| | EPZ004777 HCl Basic information |
| Product Name: | EPZ004777 HCl | | Synonyms: | 7-[5-Deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-ribofuranos;EPZ004777 HCl;EPZ004777 (hydrochloride);1-(3-((((2R,3S,4R,5R)-5-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea hydrochloride;7H-pyrrolo[2,3-d]pyrimidin-4-amine,7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylEthyl)phenyl]amino]carbonyl]amino]propyl](1-methylEthyl)amino]-β-D-ribofuranosyl]-,hydrochloride(1:1) | | CAS: | 1380316-03-9 | | MF: | C28H42ClN7O4 | | MW: | 576.14 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1380316-03-9.mol |  |
| | EPZ004777 HCl Chemical Properties |
| storage temp. | 4°C, protect from light | | solubility | insoluble in H2O; ≥16.5 mg/mL in DMSO; ≥26.35 mg/mL in EtOH | | form | Powder | | color | Light yellow to yellow |
| | EPZ004777 HCl Usage And Synthesis |
| Biological Activity | epz004777 is a potent and selective inhibitor of dot1l, a protein methyltransferase catalyzing the methylation of lysine 4 of histone h3 (h3k4), with the half maximal inhibition concentration ic50 value of 400 pm [1].epz004777 has been found to concentration-dependently inhibit the h3k79 methylation in a variety of mixed lineage leukemia (mll) cells, including mll-rearranged acute myeloid leukemia (molm-13 and mll-af9), mll-rearranged biphenotypic leukemia (mv4-11 and mll-af4) and non-mll-rearranged t cell acute leukemia cells [1].additionally, epz004777 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) [1]. | | target | DOT1L | | references | [1] daigle sr, olhava ej, therkelsen ca, majer cr, sneeringer cj, song j, johnston ld, scott mp, smith jj, xiao y, jin l, kuntz kw, chesworth r, moyer mp, bernt km, tseng jc, kung al, armstrong sa, copeland ra, richon vm, pollock rm. selective killing of mixed lineage leukemia cells by a potent small-molecule dot1l inhibitor. cancer cell. 2011 jul 12;20(1):53-65. doi: 10.1016/j.ccr.2011.06.009. |
| | EPZ004777 HCl Preparation Products And Raw materials |
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