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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-c-Myc-MYCi975
MYCi975

Chemical Structure : MYCi975

CAS No.: 2289691-01-4

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MYCi975 (NUCC-0200975, MYCi 975)

货号: PC-73127Not For Human Use, Lab Use Only.

MYCi975 (NUCC-0200975) is a close analog of MYCi361 with improved therapeutic index, binds to MYC protein with KD of 2.5 uM, disrupts MYC/MAX complex formation.

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5 mg ￥1880 In stock
10 mg ￥2980 In stock
25 mg ￥4880 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MYCi975 (NUCC-0200975) is a close analog of MYCi361 with improved therapeutic index, binds to MYC protein with KD of 2.5 uM, disrupts MYC/MAX complex formation.
MYCi975 (8 uM) enhances MYC degradation and phosphorylation on T58 in treated cells, also directly increases GSK3β-mediated MYC pT58 in the in vitro kinase assay at 6 uM.
MYCi975 inhibits MYC-dependent cancer cell viability and suppresses MYC transcriptional activity.
MYCi975 increases tolerability at significantly higher doses.
MYCi975 exhibits excellent pharmacokinetic profiles following p.o., i.p. or i.v. administration.
MYCi975 (100 mg/kg/day) inhibits tumor growth in MycCaP allografts with no changes in body weight.
MYCi975 synergized with Ara-C with no obvious impact in NSG mice bearing MV-411 AML xenografts.

物理化学性质&存储条件

分子量 561.31
分子式 C25H16Cl2F6N2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4'-chloro-6-((4-chlorobenzyl)oxy)-3-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl)-3'-(trifluoromethyl)-[1,1'-biphenyl]-2-ol

参考文献

1. Han H, et al. Cancer Cell. 2019 Nov 11;36(5):483-497.e15.

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