| Company Name: |
Jilin Province Woda Biotechnology Co., Ltd.
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| Tel: |
13504435624 |
| Email: |
1927928688@qq.com |
| Products Intro: |
Product Name: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...
CAS:2407452-77-9
Purity:99% HPLC Package:1克;5克;
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| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
4008200310 |
| Email: |
marketing@tsbiochem.com |
| Products Intro: |
Product Name:MS67
CAS:2407452-77-9
Package:25mg/RMB 16600;50mg/RMB 25100;100mg/RMB 38100
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| Product Name: | MS67 | | 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 | | CAS: | 2407452-77-9 | | MF: | C52H59F4N9O7S | | MW: | 1030.14 | | EINECS: | | | Product Categories: | | | Mol File: | 2407452-77-9.mol |  |
| Boiling point | 1134.6±65.0 °C(Predicted) | | density | 1.325±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: 2mg/mL, clear | | form | Solid | | pka | 8.27±0.10(Predicted) | | color | White to off-white |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| Uses | 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]. | | 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]. | | in vivo | 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]. | Animal Model: | MV4;11 MLL-r AML xenograft mouse[1] | | Dosage: | 75 mg/kg | | Administration: | i.p.; twice daily; 5 days a week; for 20 days | | Result: | Inhibited tumor growth in vivo. |
| | IC 50 | VHL; WDR5: 63 nM (Kd) | | 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. |
| | MS67 Preparation Products And Raw materials |
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