Lys-PEG1-Dasa
Lys-PEG1-Dasa is a BCR-ABL PROTAC degrader with an DC50 of 0.98 nM in K562 cells. Lys-PEG1-Dasa exerts growth inhibitory with IC50 of 0.4569 nM in K562 cells. Lys-PEG1-Dasa can be used for chronic myeloid leukemia research.
(Pink: Bcr-Abl ligand (HY-10181); Blue: Ligands for E3 Ligase ligand (HY-N0469); Black: linker).
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- Formule: C33H47ClN10O5S
- Masse moléculaire:731.31
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Lys-PEG1-Dasa (0-2.5 nM, 0-48 h) efficiently downregulates BCR-ABL and exerts potent antiproliferative activity in K562 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 cells
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Concentration:0, 0.01, 0.1, 0.25, 0.5, 0.75, 1 and 2.5 nM
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Incubation Time:48 h
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Result:Exerted potent antiproliferative activity with IC50 = 0.4569 nM
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Cell Line:K562 cells
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Concentration:0, 0.5, 1, 2.5 and 5 nM
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Incubation Time:0, 12, 24, 36 and 48 h
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Result:Efficiently downregulated BCR-ABL protein expression with DC50 = 0.4790 nM, Dmax = 99.1% at 5 nM.
Chemical Information
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Masse moléculaire 731.31
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Formule C33H47ClN10O5S
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SMILES
CC1=CC=CC(Cl)=C1NC(C2=CN=C(NC3=CC(N4CCN(CCOC(CCOCCNC([C@H](CCCCN)N)=O)=O)CC4)=NC(C)=N3)S2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Chen X, et al. Mighty mini-PROTACs: an emerging class of degraders. Eur J Med Chem. 2026 Jan 5;301:118202. [Content Brief]
[2]. Zhang J, et al. Single amino acid-based PROTACs trigger degradation of the oncogenic kinase BCR-ABL in chronic myeloid leukemia (CML). J Biol Chem. 2023 Aug;299(8):104994. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)