MYCi361
- Product Name
- MYCi361
- CAS No.
- 2289690-31-7
- Chemical Name
- MYCi361
- Synonyms
- MYCi361;NUCC-0196361;MYCi361 ,S8905;MYCi361 (NUCC-0196361);c-Myc,NUCC0196361,MYCi 361,MYCi361,MYCi-361,NUCC 0196361,inhibit,Inhibitor,Myc;2-[3,5-bis(trifluoromethyl)phenyl]-3-[(4-chlorophenyl)methoxy]-6-[2-methyl-5-(trifluoromethyl)pyrazol-3-yl]phenol;6-((4-Chlorobenzyl)oxy)-3-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl)-3',5'-bis(trifluoromethyl)-[1,1'-biphenyl]-2-ol;[1,1'-Biphenyl]-2-ol, 6-[(4-chlorophenyl)methoxy]-3-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]-3',5'-bis(trifluoromethyl)-
- CBNumber
- CB25821226
- Molecular Formula
- C26H16ClF9N2O2
- Formula Weight
- 594.86
- MOL File
- 2289690-31-7.mol
MYCi361 Property
- storage temp.
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- DC32581
- Product name
- MYCi361
- Packaging
- 100mg
- Price
- $700
- Updated
- 2021/12/16
- Product number
- DC32581
- Product name
- MYCi361
- Packaging
- 250mg
- Price
- $1150
- Updated
- 2021/12/16
- Product number
- DC32581
- Product name
- MYCi361
- Packaging
- 1g
- Price
- $2500
- Updated
- 2021/12/16
MYCi361 Chemical Properties,Usage,Production
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.. |
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
MYCi361 Preparation Products And Raw materials
Raw materials
Preparation Products
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