abl-1

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

ON 146040 is an effective inhibitor of PI3K isoforms with IC50s of 14 and 20 nM for PI3Kα and PI3Kδ, respectively.

Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.

Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.

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.

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

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

Imatinib impurities3 is a protein kinases inhibitor with IC50 values of 6.95uM, 0.245uM, 0.139uM for ABL1 wt, KIT wt, PDGFRR wt, respectively.

Gypsogenin (639-14-5) is a naturally occurring biochemical that shows anti-ABL1 kinase and anti-chronic Myelogenous Leukemia activities.

PPY A is a potent inhibitor of T315l mutant and wild-type Abl kinase (IC50 of 9 and 20 nM, respectively).PPY A also inhibits the growth of Bcr-Abl T315l mutant or wild-type Bcr-Abl genetically transformed cells.

AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).

BCR-ABL1-IN-1 is a highly potent, orally bioavailable inhibitor with remarkable specificity towards ABL kinase, showing significant promise for elucidating the precise role of ABL kinases in the central nervous system, particularly in preclinical investigations [1].

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

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].

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

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

Agerafenib hydrochloride, a highly potent inhibitor of BRAFV600E (Kd: 14 nM), demonstrates significant efficacy.

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5 nM for TRKA, 0.7 nM for TRKB, and 2.6 nM for TRKC. The compound demonstrates good selectivity within the kinase group and exhibits significant anti-tumor efficacy in vivo.

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

LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.

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

ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1), with IC50 values of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.

BIX02188 is a selective and potent MEK5 inhibitor that inhibits MEK5-induced apoptosis in cells expressing the oncogenic mutant FLT3-ITD.

Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI) exhibiting antiproliferative activity against the chronic myeloid leukemia (CML) cell line K562, with a CC50 of 0.8 µM. Tyrosine kinase-IN-8 is applicable for research in chronic leukemia.