Bcr-Abl

BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia.

CZC-8004 (CZC-00008004) (CZC-00008004), an aminopyrimidine, is a pan-kinase inhibitor. CZC-8004 (CZC-00008004) can bind a range of tyrosine kinases, including EGFR and VEGFR2 with IC50 values of 650 and 437 nM, respectively.

BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.

Bafetinib is a dual Bcr-Abl/Lyn tyrosine kinase inhibitor.

Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.

CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.

CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities.

A potent and dual AblWT/Src inhibitor

DPH is a cell-permeable, small-molecule activator of c-Abl kinase.

GMB-475 is a degrader of BCR-ABL1 tyrosine kinase 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 the oncogenic fusion protein.

ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).

Bosutinib-d8 is intended for use as an internal standard for the quantification of bosutinib by GC- or LC-MS.

An internal standard for the quantification of ponatinib

Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.

SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.

Lyn-IN-1 (Bafetinib analog) is a highly active dual inhibitor of Bcr-Abl and Lyn.

Vamotinib (PF-114) is an effective, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the self-phosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib exhibits anti-proliferative and anti-tumor activity. Vamotinib has potential in the study of resistant Philadelphia chromosome-positive (Ph+) leukemia.

HG-7-86-01 (Compound 26) is type II tyrosine kinase inhibitor.

PD173952 is a tyrosine kinases inhibitor with IC50s of 0.3, 1.7 and 6.6 nM against Lyn, Abl and Csk, respectively.

Risvodetinib (IkT-148009) is an oral, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM.

SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM.

PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoetl linker.

BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor containing trimethoxy group.

AKE-72 (compound 5) is a potent inhibitor of Pan-BCR-ABL.