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

CAS No.: 2289690-31-7

MYCi361 Catalog No. CSN27191

Synonyms: NUCC-0196361

MYCi361 is a MYC inhibitor with Kd value of 3.2μM. It engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 suppressed in vivo tumor growth in mice, increased tumor immune cell infiltration, upregulated PD-L1 on tumors, and sensitized tumors to anti-PD1 immunotherapy.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

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. MYCi361 is an inhibitor of MYC that binds to intracellular MYC with a K_D of 3.2 μM. Treatment of PC3 cells with MYCi361 (4–10 μM; 0.5 hr) led to significant thermal destabilization of MYC protein. Treatment of PC3 cells with MYCi361 (6 μM; 1 hr) led to disruption of the MYC/MAX interaction. MYCi361 (6 μM) decreased MYC protein stability by modulating MYC-Threonine 58 phosphorylation in PC3 cells. MYCi361 (6 μM; 24 h) also potently suppressed the expression of MYC target genes CDC25A and MYB in MYCT58A-expressing cells. MYCi361 inhibited the viability of MYC-dependent cancer cells including prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2) with low-micromolar IC₅₀ values. MYCi361 treatment of FVB mice bearing established MycCaP tumor allografts at 100 mg/kg/day induced tumor regression^[2].
作用机制MYCi361 binds to amino acids 366–378 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
- 1.6811 mL
- 8.4054 mL
- 16.8108 mL
- 5 mM
- 0.3362 mL
- 1.6811 mL
- 3.3622 mL
- 10 mM
- 0.1681 mL
- 0.8405 mL
- 1.6811 mL

技术信息

CAS号

2289690-31-7

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

C26H16ClF9N2O2

运输

蓝冰

分子量

594.86

别名

NUCC-0196361

溶解度

DMSO	100.0 mg/mL (168.1 mM)
Water	Insoluble
Ethanol	14.0 mg/mL (23.5 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

MYCi361 Catalog No. CSN27191

靶点选择性

请登录您的专属账户

确认信息