bcr-abl1

GMB-475, also known as PROTAC BCR-ABL1 ligand 1, allosterically targets and binds to the BCR-ABL1 protein. It effectively recruits the E3 ligase Von Hippel-Lindau, leading to the ubiquitination and subsequent degradation of BCR-ABL1 [1].

PROTAC BCR-ABL1 ligand 1 is the ligand of PROTAC .

BCR-ABL1-IN-1 is a highly potent and orally bioavailable inhibitor, displaying remarkable specificity towards ABL kinase. Notably, this compound holds significant promise for delineating the precise involvement of ABL kinases within the central nervous system, particularly in preclinical investigations [1].

(S,R,S)-AHPC TFA (VHL ligand 1 TFA) (VH032-NH2 TFA) is a VH032-based ligand designed for von Hippel-Lindau (VHL) protein recruitment. This compound can be linked to protein ligands (e.g., BCR-ABL1) using a linker to create PROTACs (e.g., GMB-475), which effectively induce the degradation of BCR-ABL1, demonstrated by an IC50 of 1.11 μM in Ba/F3 cells.

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

DCC-2036 (Rebastinib (DCC-2036)) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FLT3, KDR, and Tie-2, and low activity to c-Kit. Rebastinib aimed at the Angiopoietin2-Tie2 pathway.

GMB-475 is a BCR-ABL1 tyrosine kinase degrader based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL).resulting in ubiquitination and subsequent degradation of th

Radotinib (IY-5511), and sometimes referred to by its investigational name IY5511, is a drug for the treatment of different types of Y, most notably Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) with resistance or intolerance of other tyrosine kinase Bcr-Abl inhibitors

BP-5-087 is a STAT3 inhibitor, combining with BCR-ABL1 inhibition to overcome kinase-independent resistance in chronic myeloid leukemia.

BCR-ABL-IN-2 is a BCR-ABL1 tyrosine kinase inhibitor (IC50s: 57 nM, 773 nM for ABL1 native and ABL1 T315I).

CHMFL-ABL-053 (Compound 18a) is a potent, selective, and orally available BCR-ABL, SRC and p38 kinase inhibitor with IC 50 values of 70, 90 and 62 nM against ABL1, SRC and p38, respectively. CHMFL-ABL-053 is a potentially useful drug candidate for Chronic Myeloid Leukemia(CML)[1].

Vodobatinib (K-0706) is a novel 3rd generation (3G) TKI effective against wild-type and mutated BCR-ABL1 with limited off-target activity.

Asciminib (ABL001) hydrochloride is a selective and potent mutant BCR-ABL1 inhibitor that inhibits Ba/F3 cell growth (IC50: 0.25 nM).