| Identification | Back Directory | [Name]
MS4077 | [CAS]
2230077-10-6 | [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]- | [Molecular Formula]
C55H72ClN9O13S | [MDL Number]
MFCD31812631 | [MOL File]
2230077-10-6.mol | [Molecular Weight]
1134.73 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | [IC 50]
ALK; Cereblon | [storage]
Store at -20°C, sealed storage, away from moisture and light | [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. |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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