| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310 |
| Email: |
3003867561@qq.com |
| Products Intro: |
Product Name:MS4077
CAS:2230077-10-6
Purity:98% Package:5mg；10mg；20mg；50mg；100mg；200mg
|
|
| Product Name: | MS4077 | | Synonyms: | MS4077;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]-;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 | | CAS: | 2230077-10-6 | | MF: | C55H72ClN9O13S | | MW: | 1134.73 | | EINECS: | | | Product Categories: | | | Mol File: | 2230077-10-6.mol |  |
| | MS4077 Chemical Properties |
| density | 1.318±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C, sealed storage, away from moisture and light | | solubility | DMSO : 110 mg/mL (96.94 mM; Need ultrasonic) | | form | Solid | | pka | 10.74±0.40(Predicted) | | color | Yellow to green |
| | MS4077 Usage And Synthesis |
| 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 |
|