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).
For research use only. We do not sell to patients.
- Formula: C33H47ClN10O5S
- Molecular Weight:731.31
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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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
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. Further protocols information, click here.
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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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Molecular Weight 731.31
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Formula 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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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 Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[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)
Lys-PEG1-Dasa Related Classifications
HY-180963 Related Classifications
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