MS4077

Product Name: 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
Formula Weight: 1134.73
MOL File: 2230077-10-6.mol

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MS4077 Property

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

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Hazard and Precautionary Statements (GHS)

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MS4077 Chemical Properties,Usage,Production

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

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

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MS4077 Suppliers

China 9 United States 2 Global 11

Jilin Province Woda Biotechnology Co., Ltd.

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TargetMol Chemicals Inc.

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TargetMol Chemicals Inc.

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Adooq Bioscience LLC

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Henan Inokai New Materials Co., Ltd

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2230077-10-6, MS4077Related Search:

1H-Isoindole-1,3(2H)-dione, 4-[[2-[4-[6-[(6-acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]-2-oxoethyl]amino]-2-(2,6-dioxo-3-piperidinyl)- MS4078 MS1943

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

2230077-10-6

C55H72ClN9O13S