Bcr-Abl Degrader

SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC₅₀ value of 2.7 nM. SIAIS100 TFA can be used to research chronic myeloid leukemia (CML).

PROTAC BCR-ABL Degrader-1 is a PROTAC degrader targeting BCR-ABL, and also selectively inhibits cancer cell proliferation. PROTAC BCR-ABL Degrader-1 induces degradation via the ubiquitin-proteasome system to reduce protein levels. PROTAC BCR-ABL Degrader-1 can be used for research on chronic myeloid leukemia.

Asciminib-NH2 is a BCR-ABL ligand and can be used for the synthesis of PROTACs, such as P19As (HY-180981).

Azo-PROTAC-4C-cis is a BCR-ABL PROTAC degrader, and its degradation efficiency of BCR-ABL is much lower than that of its trans isomer Azo-PROTAC-4C-trans (HY-180983). Azo-PROTAC-4C-cis is the product of the conformational transformation of Azo-PROTAC-4C-trans under ultraviolet (UV) light irradiation. Azo-PROTAC-4C-cis can be converted into highly active Azo-PROTAC-4C-trans under visible light, thereby initiating protein degradation. Azo-PROTAC-4C-cis can be used for the study of myeloid leukemia.

GMB-805 is a BCR-Abl PROTAC degrader with a DC₅₀ of 30 nM in K562 cells. GMB-805 exerts antiproliferative activity in K562 cells. GMB-805 exhibits potent anti-tumor activity with favorable safety profile in vivo. GMB-805 can be used for chronic myeloid leukemia research.

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.

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.

SIAIS056 is a BCR-ABL PROTAC degrader with a DC₅₀ value of 0.18 nM. SIAIS056 time-dependently inhibits the BCR-ABL signaling pathway, accompanied by decreased phosphorylation of BCR-ABL and the downstream molecules STAT5 and CRKL in K562 cells. SIAIS056 induces the degradation of several clinically relevant resistance-conferring mutations of BCR-ABL. SIAIS056 exhibits anti-proliferative activity and induces substantial tumor regression in K562 xenograft models. SIAIS056 can be used for leukemia research.

P22D is a BCR-ABL PROTAC degrader based on Dasatinib (HY-10181), with a DC₅₀ value of approximately 10 nM for the wild-type BCR-ABL protein. P22D cannot degrade the BCR-ABL T315I mutant. P22D has inhibitory activity against K562 cells (wild type), but is ineffective against BaF3-BCR-ABL (T315I) cells. P22D can be used for research on chronic myeloid leukemia and acute lymphocytic leukemia.

Azo-PROTAC-4C-trans is a BCR-ABL PROTAC degrader that can efficiently degrade the BCR-ABL fusion protein and ABL protein. Azo-PROTAC-4C-trans exhibits potent selective anti-proliferative activity against K562 cells. Azo-PROTAC-4C-trans allows real-time, reversible regulation of its activity via UV (to inactivate it) /visible light (to activate it) irradiation. Azo-PROTAC-4C-trans can be used for the study of myeloid leukemia.

Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, with its DC₅₀ being 1.56 nM. Phe-PEG1-Dasa uses a single amino acid (Phe) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, thus being called a mini-PROTAC. Phe-PEG1-Dasa significantly inhibits the proliferation of K562 cells. Phe-PEG1-Dasa can be used for the study of leukemia.

Leu-PEG1-Dasa is a potent BCR-ABL PROTAC degrader with a DC₅₀ of 0.48 nM. Leu-PEG1-Dasa uses a single amino acid as the E3 ligand and belongs to a mini-PROTAC, functioning through the N-terminal canonical pathway. Leu-PEG1-Dasa exhibits potent anti-proliferative activity against K562 cells. Leu-PEG1-Dasa can be used for the study of chronic myeloid leukemia (CML).

DS-PPE-GW is a BCR-ABL ATTEC degrader. DS-PPE-GW connects BCR-ABL and LC3B, thereby tethering BCR-ABL to the autophagosome membrane. DS-PPE-GW shows potent BCR-ABL degradation. DS-PPE-GW has anticancer activity against chronic myeloid leukemia (Pink: LC3B ligand (HY-10542); Blue: BCR-ABL ligand (HY-107447); Black: Linker (HY-W001860)).

BCR-ABL degrader 1 (Compound 23) is a HyT-based BCR-ABL degrader with a DC₅₀ of 19.9 μM. BCR-ABL degrader 1 can be used in the research of chronic myeloid leukemia.

PROTAC DDa-1 is a multi-targeted DCAF1-recruiting tyrosine kinase PROTAC degrader. PROTAC DDa-1 mediates the degradation of TNK2, CSK, LIMK2, TEC, and BTK, with a DC₅₀ of 90 nM for BTK. PROTAC DDa-1 reduces the viability of BTK-dependent diffuse large B-cell lymphoma cells. PROTAC DDa-1 can be used for the research of diffuse large B-cell lymphoma.

PROTAC BCR-ABL Degrader-2 is a selective Bcr-Abl^T315 PROTAC degrader with a DC₅₀ of 108.7 nM in Ba/F3 Bcr-Abl^T315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research.

Arg-PEG1-Dasa is a mini-PROTAC targeting BCR-ABL. Arg-PEG1-Dasa induces BCR-ABL degradation (EC₅₀ = 0.85 nM) and shows antiproliferative activity in K562 cells (IC₅₀ = 0.36 nM). Arg-PEG1-Dasa can be used for chronic myeloid leukemia research.

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.

SIAIS100 is a potent BCR-ABL PROTAC degrader with an DC₅₀ value of 2.7 nM. SIAIS100 can be used to research chronic myeloid leukemia (CML).

ML 2-23 is a PROTAC degrader that recruits RNF114 to target BCR-ABL/c-ABL for degradation. ML 2-23 promotes proteasome-dependent degradation of the target protein and inhibits phosphorylation of downstream CRKL. At concentrations used for BCR-ABL degradation, ML 2-23 only causes slight impairment to the viability of cancer cells. ML 2-23 can be used in the research of chronic myeloid leukemia.