MYCi975 (NUCC-0200975)|CAS 2289691-01-4|DC Chemicals

Cas No.:	2289691-01-4
Chemical Name:	4'-chloro-6-((4-chlorobenzyl)oxy)-3-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl)-3'-(trifluoromethyl)-[1,1'-biphenyl]-2-ol
Synonyms:	MYCi975; MYCi975; MYCi975; NUCC-0200975; NUCC0200975; NUCC 0200975;
SMILES:	ClC1C([H])=C([H])C(=C([H])C=1C(F)(F)F)C1=C(C([H])=C([H])C(=C1O[H])C1=C([H])C(C(F)(F)F)=NN1C([H])([H])[H])OC([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])Cl
Formula:	C₂₅H₁₆Cl₂F₆N₂O₂
M.Wt:	561.3054
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[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.

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].
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].
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].

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