INDEX NAME NOT YET ASSIGNED
- CAS No.
- 2407452-77-9
- Chemical Name:
- INDEX NAME NOT YET ASSIGNED
- Synonyms
- MS67;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-((3R,5S)-3,4,5-trimethylpiperazin-1-yl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carbo...;N-{2'-fluoro-5'-[({[(2S)-1-[(2S,4R)-4-hydroxy-2-{[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl}pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl}methyl)carbamoyl]-4-[(3R,5S)-3,4,5-trimethylpiperazin-1-yl]-[1,1'-biphenyl]-3-yl}-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
- CBNumber:
- CB59770206
- Molecular Formula:
- C52H59F4N9O7S
- Molecular Weight:
- 1030.15
- MDL Number:
- MOL File:
- 2407452-77-9.mol
INDEX NAME NOT YET ASSIGNED Chemical Properties,Uses,Production
Biological Activity
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects[1]. MS67 (0.001-1 μM) induces WDR5 degradation at a concentration as low as 1 nM. MS67 induces WDR5 depletion much more effectively in all six mixed lineage leukemia (MLL)-r acute myeloid leukemia (AML) and four pancreatic ductal adenocarcinoma (PDAC) cell lines without a hook effect and in a concentration-dependent manner in PDAC cells[1].MS67 decreases H3K4me2/3 in both MV4;11 and MIA PaCa-2 cells, whereas other examined histone methylation marks such as H3K9me3, H3K27me3, and H3K36me3 are not affected . MS67 is effective in suppressing both WDR5-related gene expression programs and WDR5/MLL-induced H3K4 methylations on chromatin[1].The GI50 values of MS67 in the two most sensitive AML lines, MV4;11 and EOL-1, are 15 nM and 38 nM, respectively. MLL-r acute leukemia cell lines including MV4;11, EOL-1, MOLM13, KOPN8, RS4;11, and THP-1 are sensitive to MS67, whereas leukemia cell lines that did not harbor MLL-r (including K562, HL60, and a murine AML line transformed by Hoxa9 plus Meis1) are insensitive to MS67[1]..MS67 binds to VCB (VHL-Elongin C-Elongin B ternary complex), with a Kd of 140 nM[1]. MS67 (75 mg/kg; i.p.; twice daily; 5 days a week; for 20 days) significantly inhibits tumor growth in vivo and prolongs survival of the treated mice[1].After a single intraperitoneal (i.p.) injection of MS67 at a dose of 75 mg/kg, the Cmax reached at about 4.2 μM, and the concentration of MS67 retained above 0.5 μM over 12 hours[1].
References
[1]. Xufen Yu, et al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.
INDEX NAME NOT YET ASSIGNED Preparation Products And Raw materials
Raw materials
Preparation Products
INDEX NAME NOT YET ASSIGNED Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3466 | 58 |
| Jilin Province Woda Biotechnology Co., Ltd. | 13504435624 | 1927928688@qq.com | China | 1385 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24647 | 58 |
| Suzhou Zhongke New Drug Basket Biomedical Technology Co., Ltd. | 13616278204 | shenlei@supharm.cn | China | 88 | 58 |
| Shanghai Easy CDMO Co.,Ltd | 021-61734564 | August@easycdmo.com | China | 10010 | 58 |
| Jilin Chinese Academy of Sciences-yanshen Technology | 18143011203 | ET-market@chemextension.com | China | 24649 | 58 |
| Elucigen bio | 13501719342 | wayne.zheng@elucigenbio.com | China | 4587 | 58 |