|4'-氯-6-((4-氯苄基)氧基)-3-(1-甲基-3-(三氟甲基)-1H-吡唑-5-基)-3'-(三氟甲基)-[1,1'-联苯]-2-醇|CsnPharm

CAS No.: 2289691-01-4

4'-Chloro-6-((4-chlorobenzyl)oxy)-3-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl)-3'-(trifluoromethyl)-[1,1'-biphenyl]-2-ol Catalog No. CSN27192

Synonyms: NUCC-0200975

MYCi975 improved analog of MYCi361 which is a MYC inhibitor. It showed better tolerability compared with MYCi361.

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技术信息

生物活性

描述MYC proteins, including MYC, MYCL, and MYCN, play critical roles in tumorigenesis and therapeutic resistance. MYCi975 is an inhibitor of MYC that binds to intracellular MYC with a K_D of 2.5 μM. Treatment of PC3 cells with MYCi975 (8 μM) enhanced MYC degradation and phosphorylation on T58. MYCi975 (6 μM) directly increased GSK3β-mediated MYC pT58 in the in vitro kinase assay. In prostate cancer cells and PC12 cells, MYCi975 inhibited cell viability in an MYC-dependent manner and selectively suppressed E-box luciferase activity. MYCi975 (6 μM; 24 h) affected the expression of 3,647 genes, most (69%) of which were MYC responsive. In vivo, MYCi975 significantly inhibited tumor growth and increased survival in the MycCaP allograft model with animals tolerating a 100 mg/kg/day i.p. dosing for 14 days. It increased pT58 and PD-L1 levels and enhanced tumor infiltration of CD3⁺ T cells, B220⁺ B Cells, and NKp46⁺ NK cells. Moreover, treatment of Lewis lung carcinoma (LLC1)-bearing mice with MYCi975 (100 mg/kg/day) inhibited tumor growth with no changes in body weight^[2].
作用机制MYCi975 binds to amino acids 353–439 of the MYC protein^[2].
参考文献

[1] Han H, Jain AD, Truica MI, et al. Small-Molecule MYC Inhibitors Suppress Tumor Growth and Enhance Immunotherapy. Cancer Cell. 2019;36(5):483-497.e15. doi:10.1016/j.ccell.2019.10.001
[2] Han H, et al. Small-Molecule MYC Inhibitors Suppress Tumor Growth and Enhance Immunotherapy. Cancer Cell. 2019 Nov 11;36(5):483-497.e15

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7816 mL
- 8.9078 mL
- 17.8157 mL
- 5 mM
- 0.3563 mL
- 1.7816 mL
- 3.5631 mL
- 10 mM
- 0.1782 mL
- 0.8908 mL
- 1.7816 mL

技术信息

CAS号

2289691-01-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H16Cl2F6N2O2

运输

蓝冰

分子量

561.30

别名

NUCC-0200975

溶解度

DMSO	100.0 mg/mL (178.2 mM)
Water	Insoluble
Ethanol	60.0 mg/mL (106.9 mM)

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4'-Chloro-6-((4-chlorobenzyl)oxy)-3-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl)-3'-(trifluoromethyl)-[1,1'-biphenyl]-2-ol Catalog No. CSN27192

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