MYCi975

Names

[ Name ]:
MYCi975

[Synonym ]:
MFCD32263413

Biological Activity

[Description]:

MYCi975 (NUCC-0200975) is an orally active MYC inhibitor, which disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 (NUCC-0200975) exhibits potent anti-tumor efficacy with good tolerability, increases tumor immune cell infiltration, and sensitizes tumors to anti-PD1 immunotherapy[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> c-Myc

[Target]

MYC[1]

[In Vitro]

MYCi975 (3 days) inhibits P493-6, MV411, and SK-N-B2 cells viability in an MYC-dependent manner with IC50s of 3.7, 3.9, 6.4 μM, respectively[1].

[In Vivo]

MYCi975 exhibits excellent pharmacokinetic profiles following p.o., i.p., or i.v. administration. The half-lives observed are 7 and 12 hours when dosed at 100 and 250 mg/kg p.o., respectively. The Cmax values attained are 41,533 ng/mL (74 μM) and 54,000 ng/mL (96 μM), respectively[1]. MYCi975 significantly inhibits tumor growth and increases survival in the MycCaP allograft model with animals tolerating a 100 mg/kg/day i.p. dosing for 14 days[1].

[References]

[1]. Han H, et al. Small-Molecule MYC Inhibitors Suppress Tumor Growth and Enhance Immunotherapy. Cancer Cell. 2019 Nov 11;36(5):483-497.e15.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₁₆Cl₂F₆N₂O₂

[ Molecular Weight ]:
561.30

[ Storage condition ]:
-20°C