| Identification | Back Directory | [Name]
MYCi361 | [CAS]
2289690-31-7 | [Synonyms]
MYCi361
NUCC-0196361
[1,1'-Biphenyl]-2-ol, 6-[(4-chlorophenyl)methoxy]-3-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]-3',5'-bis(trifluoromethyl)- | [Molecular Formula]
C26H16ClF9N2O2 | [MDL Number]
MFCD32263412 | [MOL File]
2289690-31-7.mol | [Molecular Weight]
594.86 |
| Chemical Properties | Back Directory | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
Soluble in DMSO:110.0(Max Conc. mg/mL);184.9(Max Conc. mM) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
MYCi361 (NUCC-0196361) is a MYC inhibitor with the Kd of 3.2 μM for binding to MYC. MYCi361 (NUCC-0196361) suppresses tumor growth and enhances anti-PD1 immunotherapy[1]. | [in vivo]
MYCi361 inhibits MYC-dependent tumor growth in vivo. MYCi361 treatment (100 mg/kg/day for 2 days; then 70 mg/kg/day for 9 days) induces tumor regression in FVB or NSG male mice[1].
MYCi361 has moderate terminal elimination half-life of 44 and 20 h for intraperitoneal (i.p.) or oral (p.o.) dosing in mice, respectively[1].
MYCi361 suppresses tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy. However, MYCi361 demonstrates a narrow therapeutic index. An improved analog, MYCi975 shows better tolerability[1]. | Animal Model: | FVB or NSG male mice of 6-8 weeks of age and 25 g bearing established MycCaP tumors[1] | | Dosage: | 50 mg/kg and 70 mg/kg | | Administration: | Treatment i.p. initially at 50 mg/kg twice daily for 2 days, then 70 mg/kg/day for 9 days | | Result: | Induced tumor regression. |
| Animal Model: | C57BL/6 mice[1] | | Dosage: | 50 mg/kg (Pharmacokinetic analysis) | | Administration: | Treated p.o. or i.p.; 24 hours | | Result: | Intraperitoneal (i.p.) or oral (p.o.) dosing in mice indicated plasma half-lives of 44 and 20 h, respectively, with maximum plasma concentrations (Cmax) of 27,200 ng/mL (46 μM) i.p. and 13,867 ng/mL (23 μM) p.o.. |
| [storage]
Store at -20°C | [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. DOI:10.1016/j.ccell.2019.10.001 |
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