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EPZ004777

Cat. No. M2334
EPZ004777 Structure
Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 160  USD160 In stock
25mg USD 320  USD320 In stock
50mg USD 500  USD500 In stock
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Quality Control & Documentation
Biological Activity

EPZ004777 is a potent, selective, small-molecule inhibitor of DOT1L with IC50 of 0.4 nM. EPZ004777 selectively inhibits H3K79 methylation and blocks expression of leukemogenic genes. EPZ004777 suppressed expression of leukemogenic genes such as Hoxa cluster genes and Meis1, and selectively impaired proliferation of MLL-AF10 and CALM-AF10 transformed cells. In vivo administration of EPZ004777 leads to extension of survival in a mouse MLL xenograft model.

Customer Product Validations & Biological Datas
Source Cell Death Dis (2018). Figure 2. EPZ004777
Method Bone resorption assay
Cell Lines RAW264.7 cells
Concentrations 10 μM
Incubation Time 60 h
Results Furthermore, no significant difference was observed between the effects of treatment at 1 and 10 μM of the DOT1L inhibitors. In bone resorption assays, both EPZ5676 and EPZ004777 increased the resorption pit area at 1 and 10 μM concentrations
Chemical Information
Molecular Weight 539.67
Formula C28H41N7O4
CAS Number 1338466-77-5
Solubility (25°C) DMSO 100 mg/mL
Ethanol 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Deshpande AJ, et al. Blood. Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l.

[2] Chen L, et al. Leukemia. Abrogation of MLL-AF10 and CALM-AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1l.

[3] Daigle SR, et al. Cancer Cell. Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.

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  Catalog
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Keywords: EPZ004777 supplier, Histone Methyltransferase, inhibitors, activators


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