2230077-10-6
Chemical Structure
MS4077
- CAS No.: 2230077-10-6
- Formula:C55H72ClN9O13S
- Molecular Weight:1134.73
IUPAC Name: 2-(4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidin-1-yl)-N-(17-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12,15-pentaoxaheptadecyl)acetamide
InChIKey: VEKJQNCZEPLNJF-UHFFFAOYSA-N
SMILES: CC(C)S(C1=C(NC2=NC(NC3=C(OC(C)C)C=C(C4CCN(CC(NCCOCCOCCOCCOCCOCCNC5=C(C(N(C6C(NC(CC6)=O)=O)C7=O)=O)C7=CC=C5)=O)CC4)C(C)=C3)=NC=C2Cl)C=CC=C1)(=O)=O
Biological Activity: MS4077 is an ALK PROTAC degrader with a DC50 of 3 nM in SU-DHL-1 cells, a DC50 of 34 nM in NCI-H2228 cells, and a Kd of 37 nM. MS4077 induces the degradation of oncogenic active ALK fusion proteins via a cereblon- and proteasome-dependent pathway, and inhibits the phosphorylation of ALK and STAT3, thereby suppressing cancer cell proliferation. MS4077 is used for the research of anaplastic large cell lymphoma and non-small cell lung cancer[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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MS4077 | 99.66% | MS4077 is an ALK PROTAC degrader with a DC50 of 3 nM in SU-DHL-1 cells, a DC50 of 34 nM in NCI-H2228 cells, and a Kd of 37 nM. MS4077 induces the degradation of oncogenic active ALK fusion proteins via a cereblon- and proteasome-dependent pathway, and inhibits the phosphorylation of ALK and STAT3, thereby suppressing cancer cell proliferation. MS4077 is used for the research of anaplastic large cell lymphoma and non-small cell lung cancer. | ||||||||||||||||||||
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References
- [1]. Zhang C, et al. Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). European journal of medicinal chemistry. 2018 May 10;151:304-314. [Content Brief]
- [2]. Hu M, et al. ALK fusion promotes metabolic reprogramming of cancer cells by transcriptionally upregulating PFKFB3. Oncogene. 2022 Sep;41(40):4547-4559. [Content Brief]
- [3]. Cieślak M, et al. Cereblon-Recruiting PROTACs: Will New Drugs Have to Face Old Challenges?. Pharmaceutics. 2023 Mar 02;15(3):812.
- [4]. Sun X, et al. PROTACs: great opportunities for academia and industry. Signal transduction and targeted therapy. 2019;4:64. [Content Brief]
