P19P
P19P is a BCR-ABL PROTAC degrader based on Ponatinib (HY-12047), with a DC50 value of approximately 20 nM for the wild-type BCR-ABL protein. P19P can effectively degrade various drug-resistant mutants such as T315I, E255K, H396R, and V468F, and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19P maintains strong inhibitory activity against ABL (T315I), with a IC50 of 13.1 nM. P19P does not inhibit the formation of vascular lumens in HUVEC. P19P can be used for research on chronic myeloid leukemia and acute lymphoblastic leukemia.
(Pink: Bcr-Abl ligand (HY-12047); Blue: Cereblon ligand (HY-14658); Black: linker (HY-180978)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 2512843-74-0
- Fòrmula: C55H57F3N12O9
- Peso molecular:1087.11
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Ver todos los productos específicos de isoformas PROTACs
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Actividad biológica
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Bcr-AblWT 20 nM (DC50) |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | EC50 |
28.5 nM
Compound: 19; P19P
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Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay
Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay
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[PMID: 32657579] |
Chemical Information
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No. CAS 2512843-74-0
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Peso molecular 1087.11
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Fòrmula C55H57F3N12O9
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SMILES
O=C(C1=CC=C(C)C(C#CC2=CN=C3C=CC=NN23)=C1)NC4=CC=C(CN5CCN(CC5)C(CCCC6=CN(CCOCCOCCOCCNC7=CC=CC(C(N8C9C(NC(CC9)=O)=O)=O)=C7C8=O)N=N6)=O)C(C(F)(F)F)=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
P19P Related Classifications
HY-180977 Related Classifications
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