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Chemical Structure : MS67
CAS No.: 2407452-77-9
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $198 | In stock | |
| 10 mg | $328 | In stock | |
| 25 mg | $578 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 1030.15 | |
| Formula | C52H59F4N9O7S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Xufen Yu, et al. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.
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