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EPZ004777

Cat. No. M2334
EPZ004777 Structure
Size Price Availability Quantity
10mg USD 257 In stock
50mg USD 780 In stock
100mg USD 1240 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 539.67
Formula C28H41N7O4
CAS Number 1338466-77-5
Purity >99%
Solubility DMSO 100 mg/mL
Ethanol 100 mg/mL
Storage at -20°C
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
Rating
References

Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l.
Deshpande AJ, et al. Blood. 2013 Mar 28;121(13):2533-41. PMID: 23361907.

Abrogation of MLL-AF10 and CALM-AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1l.
Chen L, et al. Leukemia. 2013 Apr;27(4):813-22. PMID: 23138183.

Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.
Daigle SR, et al. Cancer Cell. 2011 Jul 12;20(1):53-65. PMID: 21741596.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: EPZ004777 supplier, Histone Methyltransferase, inhibitors

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