asciminib

Asciminib (ABL001) (ABL001) is a potent and selective Bcr-Abl inhibitor (Kd: 0.5–0.8nM).

Asciminib-NH2 is a BCR-ABL ligand utilized in the synthesis of PROTACs, such as P19As.

Asciminib hydrochloride is described as a "STAMP inhibitor," specifically targeting the ABL myristoyl pocket, Asciminib hydrochloride, marketed as Scemblix, are applied in research in Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) by binding to the allosteric site of wild-type ABL N-terminus, which is myristoylated, whereas the ABL fusion protein lacks this domain, enabling selective modulation of oncogenic signaling pathways and serving as a targeted therapeutic tool in hematologic cancer research.

P19As is a BCR-ABL PROTAC degrader based on Asciminib, with a DC50 of approximately 200 nM for the wild-type BCR-ABL protein. It is capable of degrading the T315I mutant and demonstrates strong antiproliferative activity in BaF3-BCR-ABL (T315I) cells. P19As is applicable for research in chronic myeloid leukemia and acute lymphoblastic leukemia.