EPZ004777 HCl

Product Name: EPZ004777 HCl
CAS No.: 1380316-03-9
Chemical Name: EPZ004777 HCl
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;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);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
CBNumber: CB62677400
Molecular Formula: C28H42ClN7O4
Formula Weight: 576.14
MOL File: 1380316-03-9.mol

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EPZ004777 HCl Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ApexBio Technology

Product number: B1581
Product name: EPZ004777HCl
Packaging: 5mg
Price: $110
Updated: 2021/12/16

ApexBio Technology

Product number: B1581
Product name: EPZ004777HCl
Packaging: 50mg
Price: $550
Updated: 2021/12/16

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EPZ004777 HCl Chemical Properties,Usage,Production

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.

EPZ004777 HCl Preparation Products And Raw materials

Raw materials

Preparation Products

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EPZ004777 HCl Suppliers

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1380316-03-9, EPZ004777 HClRelated Search:

EPZ004777 HCl

EPZ004777 (hydrochloride)

7-[5-Deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-ribofuranos

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)

1380316-03-9

C28H41N7O4HCl

Inhibitors