EPZ028862

Names

[ CAS No. ]:
1887082-53-2

[ Name ]:
EPZ028862

Biological Activity

[Description]:

EPZ028862 is a selective SMYD3 inhibitor for cancer research[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

[In Vivo]

The pharmacokinetic parameters of EPZ028862( IV: 1 mg/kg; PO: 5 mg/kg) Parameter Mouse Rat Dog Cynomolgus CLp(mL/min/kg) 79.8 32.7 13.9 21.4 CLr(mL/min/kg) 23.6 21 1.97 1.06 Vss(L/kg) 9.5 4.4 5.8 9.5 t1/2(h) 2 2.1 5.4 5.6 MRT(h) 2 59 7 7.4 tmax(h) 0.33 1 1.5 2 F(%) 100 59 70 62

[References]

[1]. Michael J Thomenius, et al. Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation. PLoS One. 2018 Jun 1;13(6):e0197372.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₃₀N₄O₄S

[ Molecular Weight ]:
422.54

Related Compounds

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