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EPZ004777

CAT: 0804-HY-15227-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-15227-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
EPZ004777 is an effective and selective DOT1L inhibitor, with IC50 being 0.4 nM. EPZ004777 reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 can be used for the study of leukemia[1][2][3].
CAS Number
1338466-77-5
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis; Histone Methyltransferase
Type
Reference compound
Related Pathways
Apoptosis; Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/epz004777.html
Purity
99.74
Solubility
DMSO : 66.67 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
NC1=C2C(N([C@H]3[C@H](O)[C@H](O)[C@@H](CN(C(C)C)CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)O3)C=C2)=NC=N1
Molecular Formula
C28H41N7O4
Molecular Weight
539.67
Precautions
H302, H315, H319, H335
References & Citations
[1]Daigle SR, et al. Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor. Cancer Cell. 2011 Jul 12;20 (1) :53-65.|[2]Chen L, et al. 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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
DOT1L

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