MS67 | WDR5 PROTAC | Probechem Biochemicals

Chemical Structure : MS67

CAS No.: 2407452-77-9

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MS67 (WDR5 degarder MS67)

货号: PC-49507Not For Human Use, Lab Use Only.

MS67 is a highly effective, selective WDR5 degrader (PROTAC), contains the E3 ligase ligand VHL-1 and WDR5 binding moiety, shows binding affinities to VCB (Kd=140 nM) and WDR5 (Kd=63 nM), potently and selectively degrades WDR5 in MLL-r AML and PDAC cells.

规格	价格	库存
5 mg	￥1980	In stock
10 mg	￥3280	In stock
25 mg	￥5780	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

MS67 is a highly effective, selective WDR5 degrader (PROTAC), contains the E3 ligase ligand VHL-1 and WDR5 binding moiety, shows binding affinities to VCB (Kd=140 nM) and WDR5 (Kd=63 nM), potently and selectively degrades WDR5 in MLL-r AML and PDAC cells.
MS67 potently and selectively degrades WDR5 in MV4;11 cells at a concentration as low as 1 nM with DC50 of 3.7 nM (Dmax=94%), and DC50 of 45 nM in MIA PaCa-2 cells.
MS67 is effective in suppressing transcription of WDR5-regulated genes and H3K4me2 on chromatin.
MS67 exhibits significant inhibition of in vitro growth in a panel of MLL-r AML lines with IC50 of 15 and 38 nM for MV4;11 and EOL-1 cells, respectively.
MS67 (75-150 mg/kg, BID, i.p.) suppresses tumor growth in MV4;11 MLL-r AML xenograft mouse model, inhibits the growth of primary AML cells and improves survival in a PDX model.

物理化学性质&存储条件

分子量	1030.15
分子式	C52H59F4N9O7S
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	N-(2'-fluoro-5'-((2-(((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethyl)carbamoyl)-4-((3S,5R)-3,4,5-trimethylpiperazin-1-yl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide

参考文献

1. Xufen Yu, et al. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.

MS67 (WDR5 degarder MS67)

生物&药学活性

物理化学性质&存储条件

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MS67 (WDR5 degarder MS67)

生物&药学活性

物理化学性质&存储条件

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