PROTAC ALK degrader-4
PROTAC ALK degrader-4 is a ALK PROTAC degrader with a DC50 of 445.25 nM. PROTAC ALK degrader-4 induces concentration- and time-dependent degradation of EML4-ALK, as well as concentration-dependent degradation of ALKF1174L. PROTAC ALK degrader-4 downregulates 390 proteins in NCI-H3122 cells, including the targets of ceritinib (ALK, IGF-1R) and downstream molecules ERK1/2 and STAT3. PROTAC ALK degrader-4 exerts antiproliferative activity in ALK-positive cancer cells. ALK degrader-4 can be used in studies related to lung adenocarcinoma.
(Pink: Anaplastic lymphoma kinase (ALK) ligand (HY-15656); Blue: Cereblon ligand (HY-179733); Black: linker).
For research use only. We do not sell to patients.
- Formula: C46H63ClN8O7S
- Molecular Weight:907.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
EML4-ALK 445.25 nM (DC50) |
In Vitro
PROTAC ALK degrader-4 (compound B8) (0.1-10000 nM; 1-48 h) induces CRBN- and ubiquitin-proteasome system-dependent degradation of EML4-ALK in NCI-H3122 cells in a dose- and time-dependent manner, with a DC50 of 445.25 nM[1].
PROTAC ALK degrader-4 induces concentration-dependent degradation of the ALKF1174L mutant in Kelly cells, and exhibits non-mutant-selective ALK degradation activity[1].
PROTAC ALK degrader-4 (24 h) exerts antiproliferative activity in NCI-H2228 and NCI-H3122 cells[1].
PROTAC ALK degrader-4 (500 nM; 24 h) causes significant downregulation of 390 proteins in NCI-H3122 cells, including ceritinib kinase targets such as ALK and IGF-1R, as well as their downstream pathway proteins ERK1/2 and STAT3 [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:NCI-H3122 cells
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Concentration:0.1, 1, 10, 100, 1000 and 10000 nM
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Incubation Time:24 h
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Result:It induced EML4-ALK in NCI-H3122 cells, with a DC50 of 445.25 nM.
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Cell Line:NCI-H3122 cells
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Concentration:100 nM
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Incubation Time:1, 2, 4, 8, 12, 24 and 48 h
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Result:Time-dependent degradation of EML4-ALK was induced in NCI-H3122 cells
Chemical Information
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Molecular Weight 907.56
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Formula C46H63ClN8O7S
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SMILES
CC1=CC(NC2=NC(NC3=CC=CC=C3S(=O)(C(C)C)=O)=C(C=N2)Cl)=C(C=C1C4CCN(CC4)CCCCCCCC(NC5(CCC5)C(NC6C(NC(CC6)=O)=O)=O)=O)OC(C)C
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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.
Protocols
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC ALK degrader-4 Related Classifications
HY-179732 Related Classifications
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