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Art. -Nr.: HY-180977

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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)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2512843-74-0
Formel: C₅₅H₅₇F₃N₁₂O₉
Molecular Weight:1087.11

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (267 KB)

P19P Chemical Structure

CAS. Nr.: 2512843-74-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: Bcr-Abl ligand (HY-12047); Blue: Cereblon ligand (HY-14658); Black: linker (HY-180978)).

IC₅₀ & Target^[1]

Bcr-Abl^WT

20 nM (DC₅₀)

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen :

Abl
Bcr-Abl

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	EC₅₀	28.5 nM Compound: 19; P19P	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	[PMID: 32657579]

Chemical Information

CAS. Nr. 2512843-74-0
Molecular Weight 1087.11
Formel C₅₅H₅₇F₃N₁₂O₉
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yang Y, et al. Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. J Med Chem. 2020 Aug 13;63(15):8567-8583. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
Chemical Information
Reinheit & Dokumentation
Verweise

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P19P

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

P19P Related Classifications

HY-180977 Related Classifications