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MS4077

CAS No.
2230077-10-6
Chemical 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]-
CBNumber:
CB35867494
Molecular Formula:
C55H72ClN9O13S
Molecular Weight:
1134.73
MDL Number:
MFCD31812631
MOL File:
2230077-10-6.mol
Last updated:2023-07-12 17:07:07

MS4077 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)
pka 10.74±0.40(Predicted)

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

Global( 9)Suppliers
Supplier Tel Email 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 9833 58
Jilin Province Woda Biotechnology Co., Ltd. 13504435624 1927928688@qq.com China 1360 58
cjbscvictory 13348960310 13348960310 3003867561@qq.com China 10011 58
Changzhou Bojia Biomedical Technology Co., Ltd. 2122619822 czbjpharma@126.com China 18488 58
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd 021-59167510 18117107507 vip@med-life.cn China 5019 58
RD International Technology Co., Limited 18024082417 market@ubiochem.com China 9180 58
Nanjing Shizhou Biology Technology Co.,Ltd 025-85560043 15850508050 cindy.huang@synzest.com China 12007 58
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]- 2230077-10-6 C55H72ClN9O13S