CG 858-Neg
CG 858-Neg (compound 13) is a negative control for Thalidomide (HY-14658)-derived PROTAC degraders, targeting BRAF and BRAFV600E with Ki values of 9.5 nM and 14.4 nM, respectively. CG 858-Neg inhibits downstream ERK phosphorylation and suppresses BRAFV600E-driven melanoma (e.g., A375 cells, IC50=492 nM) and colorectal cancer (e.g., HT-29 cells, IC50=459 nM) cells. CG 858-Neg can be used in research related to melanoma and colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 2417296-83-2
- Formula: C43H41F2N7O8S
- Molecular Weight:853.89
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cereblon |
B-RafV600E |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
492 nM
Compound: 13
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Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
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[PMID: 32223235] |
CG 858-Neg (compound 13) is unable to bind to cereblon due to partial N-methylation of the thalidomide moiety[1].
CG 858-Neg (1-1000 nM; 16 h) does not degrade BRAFV600E and partially suppresses downstream ERK phosphorylation; at 37-1000 nM, it can inhibit the phosphorylation of downstream p-ERK in A375 cells[1].
CG 858-Neg (1000 nM; 7 days) inhibits colony formation of A375 cells at concentrations of 200 nM and above[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 melanoma cells
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Concentration:1-1000 nM
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Incubation Time:16 h
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Result:Did not induce degradation of BRAF-V600E protein levels at any tested concentration; suppressed p-ERK levels in a dose-dependent manner.
Chemical Information
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CAS No. 2417296-83-2
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Molecular Weight 853.89
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Formula C43H41F2N7O8S
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SMILES
O=C(C1=C(F)C(NS(=O)(CCC)=O)=CC=C1F)C2=CNC3=NC=C(C4=CC=C(CNC(CCCCNC5=CC=C6C(N(C7C(N(C)C(CC7)=O)=O)C(C6=C5)=O)=O)=O)C=C4)C=C32
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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