MS4077
- CAS No.
- 2230077-10-6
- Chemical Name:
- MS4077
- Synonyms
- MS4077;2-(4-{4-[(5-chloro-4-{[2-(propane-2-sulfonyl)phenyl]amino}pyrimidin-2-yl)amino]-2-methyl-5-(propan-2-yloxy)phenyl}piperidin-1-yl)-N-(17-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}-3,6,9,12,15-pentaoxaheptadecan-1-yl)acetamide;1-Piperidineacetamide, 4-[4-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-2-methyl-5-(1-methylethoxy)phenyl]-N-[17-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-3,6,9,12,15-pentaoxaheptadec-1-yl]-
- CBNumber:
- CB35867494
- Molecular Formula:
- C55H72ClN9O13S
- Molecular Weight:
- 1134.73
- MDL Number:
- MFCD31812631
- MOL File:
- 2230077-10-6.mol
MS4077 Chemical Properties,Uses,Production
Biological Activity
MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 37 nM for binding affinity to ALK[1]. MS4077 effectively inhibits cancer cell proliferation. MS4077 (10-3-1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1 cells with an IC50 of 46 ± 4 nM. In comparison with SU-DHL-1 cells, the proliferation of NCI-H2228 cells is less sensitive to MS4077(10-2-100.5 μM; 3 days)[1].MS4077 potently reduces the ALK fusion protein levels and inhibits the ALK auto-phosphorylation and down-steam STAT3 phosphorylation in both SU-DHL-1 and NCI-H2228 cells in a concentration-dependent manner. In SU-DHL-1 cells, MS4077 reduces the NPM-ALK protein levels with impressive DC50 (50% degradation) value of 3±1 nM after 16-hour treatment. Over 90% of inhibition of both ALK Y1507 and STAT3 Y705 phosphorylation is achieved at the 100 nM concentration. In NCI-H2228 cells, MS4077 reduces the EML4-ALK protein levels with similar DC50 value of 34±9 nM after 16-hour treatment. At the 100 nM concentration, NCI-H2228 cells reduces more than 90% of EML4-ALK protein levels[1].
References
[1]. Zhang C, et al. Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). Eur J Med Chem. 2018 May 10;151:304-314.
MS4077 Preparation Products And Raw materials
Raw materials
Preparation Products
MS4077 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9943 | 58 |
Jilin Province Woda Biotechnology Co., Ltd. | 13504435624 | 1927928688@qq.com | China | 1382 | 58 |
cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 10000 | 58 |
Changzhou Bojia Biomedical Technology Co., Ltd. | 2122619822 | czbjpharma@126.com | China | 18488 | 58 |
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 13417589054 | trendseenbio@gmail.com | China | 9880 | 58 |
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 021-59167510 18117107507 | vip@med-life.cn | China | 5012 | 58 |
RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9268 | 58 |
Elucigen bio | 13501719342 | wayne.zheng@elucigenbio.com | China | 4587 | 58 |