1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. Bcr-Abl
  4. Bcr-Abl Degrader

Bcr-Abl Degrader

Bcr-Abl Degraders (24):

Cat. No. Product Name Effect Purity
  • HY-152036A
    SIAIS100 TFA
    Degrader 99.75%
    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).
  • HY-107447
    N-Deshydroxyethyl Dasatinib
    Degrader
    N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, Dasatinib is a multi-kinase inhibitor that potently inhibits Bcr-Abl, Src family and platelet-derived growth factor receptor kinases. N-Deshydroxyethyl Dasatinib can be used in cancer and immune disease research.
  • HY-137342
    SB1-G-187
    Degrader 98.70%
    SB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with CRBN and specific functional kinases. SB1-G-187 can be used in tumor-related research. (Pink: multi-target kinase ligand (HY-125142); Blue: CRBN ligand (HY-A0003); Black: linker).
  • HY-153415
    PROTAC BCR-ABL Degrader-1
    Degrader 98.73%
    PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoethyl linker. PROTAC BCR-ABL Degrader-1 induces Bcr-Abl degradation in a ubiquitinproteasom-dependent manner. PROTAC BCR-ABL Degrader-1 exhibits antiproliferative activity against K562 cells, and has the potential to study cancer.
  • HY-180925
    Leu-PEG1-Dasa
    Degrader
    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).
  • HY-180218
    DS-PPE-GW
    Degrader
    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)).
  • HY-180798
    BCR-ABL degrader 1
    Degrader
    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.
  • HY-180985
    Azo-PROTAC-4C-cis
    Degrader
    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.
  • HY-180968
    GMB-805
    Degrader
    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.
  • HY-180967
    PROTAC BCR-ABL Degrader-2
    Degrader
    PROTAC BCR-ABL Degrader-2 is a selective Bcr-AblT315 PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I 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.
  • HY-180982
    Asciminib-NH2
    Degrader
    Asciminib-NH2 is a BCR-ABL ligand and can be used for the synthesis of PROTACs, such as P19As (HY-180981).
  • HY-186016
    Arg-PEG1-Dasa
    Degrader
    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.
  • HY-180963
    Lys-PEG1-Dasa
    Degrader
    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.
  • HY-180981
    P19As
    Degrader
    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.
  • HY-180977
    P19P
    Degrader
    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.
  • HY-152036
    SIAIS100
    Degrader
    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).
  • HY-175437
    MRT-7612
    Degrader
    MRT-7612 (Compound 4) is a cereblon-based tyrosine kinases molecular glue degrader. MRT-7612 significantly induces HCK and LYN degradation, with week efficacy on LCK. MRT-7612 can be used for cancers like chronic myeloid leukemia, autoimmune and chronic inflammatory diseases research.
  • HY-180969
    SIAIS056
    Degrader
    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.
  • HY-175281
    SJ11646
    Degrader
    SJ11646 is a Dasatinib (HY-10181)-based LCK PROTAC degrader with a DC50 of 0.00838 pM. SJ11646 has potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples with drastically prolonged suppression of LCK signaling, and induces T-ALL apoptosis. SJ11646 binds to 51 human kinases with a high affinity (particularly ABL1, KIT, and DDR1). SJ11646 has superior antileukemic efficacy in T-ALL mice model. . Pink: LCK ligand (HY-107447); Blue: CRBN ligase ligand (HY-163169); Black: linker (HY-76667)
  • HY-180979
    P22D
    Degrader
    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.