| Identification | Back Directory | [Name]
EPZ004777 HCl | [CAS]
1380316-03-9 | [Synonyms]
EPZ004777 HCl
EPZ004777 (hydrochloride)
7-[5-Deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-ribofuranos | [Molecular Formula]
C28H42ClN7O4 | [MDL Number]
MFCD27920717 | [MOL File]
1380316-03-9.mol | [Molecular Weight]
576.14 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with an IC50 of 0.4 nM. | [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]. | [in vivo]
EPZ004777 is well tolerated and no overt toxicity is observed. Complete blood count analysis after 14 days of continuous exposure to EPZ004777 revealed a statistically significant increase in the total white blood cell count, which resulted from an increase in neutrophils, monocytes, and lymphocytes. EPZ004777 (50, 100, or 150 mg/mL) administration is well tolerated, and no significant weight loss is observed[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. |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|