1. PROTAC Protein Tyrosine Kinase/RTK
  2. PROTACs Bcr-Abl
  3. P19As

P19As is a BCR-ABL PROTAC degrader based on Asciminib (HY-104010), with a DC50 value of approximately 200 nM for the wild-type BCR-ABL protein. P19As can degrade the T315I mutant and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19As can be used for the study of chronic myeloid leukemia and acute lymphoblastic leukemia.
(Pink: Bcr-Abl ligand (HY-180982); Blue: Cereblon ligand (HY-14658); Black: linker (HY-180978)).

For research use only. We do not sell to patients.

P19As

P19As Chemical Structure

CAS No. : 2635386-55-7

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Description

P19As is a BCR-ABL PROTAC degrader based on Asciminib (HY-104010), with a DC50 value of approximately 200 nM for the wild-type BCR-ABL protein. P19As can degrade the T315I mutant and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19As can be used for the study of chronic myeloid leukemia and acute lymphoblastic leukemia[1]. (Pink: Bcr-Abl ligand (HY-180982); Blue: Cereblon ligand (HY-14658); Black: linker (HY-180978)).

IC50 & Target[1]

Bcr-AblWT

200 nM (DC50)

Cereblon

 

Cellular Effect
Cell Line Type Value Description References
BaF3 EC50
1020 nM
Compound: 14; P19As
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]
Molecular Weight

1017.43

Formula

C47H51ClF2N12O10

CAS No.
SMILES

O=C(CCCC1=CN(CCOCCOCCOCCNC2=CC=CC(C(N3C4C(NC(CC4)=O)=O)=O)=C2C3=O)N=N1)N[C@@H]5CCN(C6=NC=C(C(NC7=CC=C(OC(Cl)(F)F)C=C7)=O)C=C6C8=NNC=C8)C5

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
P19As
Cat. No.:
HY-180981
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