Bcr-Abl

Cat. No.

A30990

CAS No.

1257628-57-1

S116836

S116836 is a potent BCR-ABL tyrosine kinase inhibitor that effectively targets both wild-type and T315I BCR-ABL variants. It induces apoptosis and arrests the cell cycle in the G0/G1 phase, promoting increased reactive oxygen species (ROS) and reduced glutathione (GSH) levels in BaF3/WT and BaF3/T315I cells. Additionally, S116836 inhibits SRC, LYN, HCK, LCK, BLK, as well as receptor tyrosine kinases including FLT3, TIE2, KIT, and PDGFR-β, demonstrating significant antitumor activity. This compound also features an alkyne group, making it suitable for click chemistry applications, particularly the copper-catalyzed azide-alkyne cycloaddition (CuAAc).

Cat. No.

A32743

CAS No.

368836-72-0

LS-104

Synonyms: Tyrene CR-4

LS-104 is a non-ATP-competitive inhibitor targeting JAK2, Bcr-Abl, and FLT3. It effectively induces apoptosis in JAK2V617F-positive cells while inhibiting JAK2 autophosphorylation and downstream signaling pathways. Additionally, LS-104 demonstrates significant cytotoxic effects and inhibits the proliferation of FLT3-expressing leukemic cells. This hydroxystyryl-acrylonitrile compound holds potential for research into myeloproliferative disorders and refractory or relapsed hematologic malignancies.

Cat. No.

A32914

CAS No.

926037-85-6

Radotinib dihydrochloride

Synonyms: IY-5511 dihydrochloride

Radotinib dihydrochloride is a selective Bcr-Abl1 tyrosine kinase inhibitor with an IC50 of 34 nM, demonstrating oral bioavailability and the ability to penetrate the blood-brain barrier. This compound exhibits significant anti-tumor activity by inhibiting cell proliferation, inducing cell cycle arrest, and promoting apoptosis in tumor cells. Radotinib dihydrochloride is utilized in research related to chronic myeloid leukemia, multiple myeloma, and neurodegenerative disorders, particularly those involving prion diseases.

Cat. No.

A32969

CAS No.

2479290-65-6

CHMFL-48

CHMFL-48 is a potent BCR-ABL kinase inhibitor that effectively targets both wild-type and imatinib-resistant mutants. With IC50 values of 1 nM for ABL wild-type and 0.8 nM for the ABL T315I mutant, CHMFL-48 inhibits autophosphorylation of BCR-ABL, disrupting downstream signaling pathways involving STAT5 and CRKL. This mechanism results in cell cycle arrest and the induction of apoptosis, making CHMFL-48 a valuable tool for research focused on chronic myeloid leukemia (CML).

Cat. No.

A33039

CAS No.

1430720-10-7

HS-438

HS-438 is a potent and selective inhibitor of BCR-ABL, a fusion protein associated with chronic myeloid leukemia (CML). This compound exhibits significant antiproliferative effects, leading to reduced phosphorylation of BCR-ABL at Tyr177, and promotes apoptosis alongside G0/G1 cell cycle arrest. HS-438 demonstrates substantial antitumor activity, making it a valuable tool for investigations into CML and related therapeutic strategies.

Cat. No.

A33377

CAS No.

1332329-27-7

Debio 0617B

Debio 0617B is a multi-kinase inhibitor that targets key kinases involved in the regulation of STAT3/STAT5 signaling, including JAK, SRC, ABL, and class III/V receptor tyrosine kinases. This compound effectively reduces the maintenance and self-renewal of primary human acute myeloid leukemia (AML) CD34+ stem/progenitor cells. Additionally, Debio 0617B has demonstrated efficacy in preclinical models of STAT3-driven solid tumors, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A33588

CAS No.

228400-22-4

AFG210

AFG210 is a potent Abl kinase inhibitor with an IC50 of 330 nM, demonstrating significant inhibitory effects on additional kinases including B-Raf, C-Raf, FGFR-1, RET, and VEGF receptors. Its unique multi-target profile positions AFG210 as a valuable tool for investigating chronic myeloid leukemia and other disorders associated with aberrant Abl kinase activation. This compound facilitates research exploring targeted therapies and signaling pathways linked to these diseases.

Cat. No.

A33592

CAS No.

185039-91-2

PD166326

PD166326 is a potent Bcr/Abl kinase inhibitor with an IC50 of 8 nM for Abl tyrosine kinase and 6 nM for Src tyrosine kinase. This compound effectively blocks Bcr/Abl kinase activity, leading to the inhibition of Bcr/Abl-dependent cell proliferation and cell cycle progression. In preclinical studies, PD166326 has demonstrated the ability to reduce peripheral blood granulocytosis, alleviate splenomegaly, and prolong survival in mouse models of chronic myeloid leukemia. It serves as a valuable tool for research focused on chronic myeloid leukemia and related signaling pathways.

Cat. No.

A33594

CAS No.

2119669-71-3

Asciminib hydrochloride

Synonyms: ABL001 hydrochloride

Asciminib hydrochloride is a potent and selective allosteric inhibitor targeting BCR-ABL1. This compound demonstrates significant biological activity by inhibiting Ba/F3 cells with an IC50 of 0.25 nM. Asciminib is primarily utilized in research applications focusing on chronic myeloid leukemia and other BCR-ABL1 driven malignancies, providing valuable insight into the mechanisms of resistance and therapeutic strategies.

Cat. No.

A33598

CAS No.

1416241-23-0

Vamotinib

Synonyms: PF-114

Vamotinib is a selective and potent orally active tyrosine kinase inhibitor that targets the BCR/ABL fusion protein, including the resistant BCR/ABL-T315I variant. It effectively inhibits autophosphorylation, leading to apoptosis and demonstrating significant anti-proliferative and anti-tumor activities. With low IC50 values across various ABL kinases, Vamotinib holds promise for research applications in Philadelphia chromosome-positive leukemia. Additionally, as a click chemistry reagent featuring an alkyne group, it enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.

Cat. No.

A33601

CAS No.

2566525-18-4

AKE-72

AKE-72 is a potent Bcr-Abl inhibitor that selectively targets various BCR-ABL variants, including BCR-ABLWT, BCR-ABLT315, BCR-ABLE255K, BCR-ABLF3171, BCR-ABLH396P, and BCR-ABLQ252H, exhibiting IC50 values of less than 0.5 nM to 9 nM. This compound demonstrates significant anti-leukemic activity in the K-562 cell line, making it a valuable tool for research in hematological malignancies and targeted cancer therapies. AKE-72 holds potential for further studies investigating BCR-ABL-mediated signaling pathways and resistance mechanisms.

Cat. No.

A33603

CAS No.

1488090-21-6

BCR-ABL1-IN-1

BCR-ABL1-IN-1 is a selective ABL1 inhibitor with an IC50 of 8.7 nM. This compound is primarily utilized in research investigating diseases of the central nervous system (CNS). Its potent inhibitory action on ABL1 makes it an invaluable tool for studying ABL-related signaling pathways and their implications in various neurological disorders.

Cat. No.

A33605

CAS No.

875634-01-8

PPY-A

PPY-A is an effective inhibitor of both wild-type and T315I mutant Abl kinases, exhibiting IC50 values of 9 nM and 20 nM, respectively. This compound also demonstrates inhibitory activity in Ba/F3 cells transformed with wild-type Abl and the T315I mutant, with IC50s of 390 nM and 180 nM, respectively. PPY-A is particularly relevant for research in chronic myeloid leukemia (CML), offering a valuable tool for investigating therapeutic strategies against this malignancy.

Cat. No.

A33609

CAS No.

688050-42-2

BCR-ABL-IN-7

BCR-ABL-IN-7 is a selective inhibitor of ABL kinases, including both wild-type and the T315I mutant forms. This compound demonstrates potent inhibitory activity against ABL kinases, making it a valuable tool in the study of chronic myeloid leukemia (CML). Researchers can utilize BCR-ABL-IN-7 to investigate mechanisms of resistance and explore therapeutic strategies in CML treatment.

Cat. No.

A33611

CAS No.

1808288-49-4

BCR-ABL-IN-8

BCR-ABL-IN-8 is a potent inhibitor of the BCR-ABL fusion protein. This compound features a trimethoxy group that enhances its activity against chronic myeloid leukemia (CML) cells. BCR-ABL-IN-8 can be utilized in research investigating the molecular mechanisms of CML and potential therapeutic strategies targeting BCR-ABL signaling pathways.

Cat. No.

A33614

CAS No.

2489876-34-6

PROTAC BCR-ABL1 ligand 1

PROTAC BCR-ABL1 ligand 1, also known as compound GMB-475, is designed to selectively target the BCR-ABL1 oncoprotein. It functions as an allosteric inhibitor by recruiting the E3 ligase Von Hippel-Lindau, leading to the ubiquitination and subsequent degradation of BCR-ABL1. This mechanism of action supports research applications in cancer biology, particularly in studying resistance mechanisms in chronic myeloid leukemia (CML) and therapeutic strategies to overcome BCR-ABL1-mediated signaling.

Cat. No.

A33616

CAS No.

2240191-12-0

BCR-ABL-IN-3

BCR-ABL-IN-3 is a potent and irreversible inhibitor of the Bcr-Abl tyrosine kinase, exhibiting an IC50 of ≤100 nM against Ba/F3Bcr-AblT3151 cells. This compound demonstrates significant anti-cancer activity, making it valuable for research applications focused on chronic myeloid leukemia and other malignancies driven by Bcr-Abl mutations. Its use can aid in elucidating the molecular mechanisms of resistance and the development of targeted therapies.

Cat. No.

A33617

CAS No.

2304918-82-7

c-ABL-IN-1

c-ABL-IN-1 is a selective inhibitor of c-Abl kinase, which plays a critical role in various cellular processes, including cell proliferation and survival. This compound demonstrates significant neuroprotective effects, making it a valuable tool in researching therapies for neurodegenerative diseases such as Parkinson's disease. Its ability to inhibit c-Abl specifically allows for targeted studies into the mechanisms underlying neurodegeneration and potential therapeutic interventions.

Cat. No.

A33619

CAS No.

2941512-37-2

DosatiLink-1

DosatiLink-1 is a selective inhibitor of the Abelson murine leukemia (ABL) enzyme. It exhibits potent inhibitory activity against ABL, making it a valuable tool for studying ABL-related signaling pathways and its role in oncogenesis. This compound is useful in research focused on cancer biology and can aid in the development of targeted therapies for ABL-driven malignancies.

Cat. No.

A33621

CAS No.

309760-28-9

WB-BC-15

Synonyms: WGB-BC-15

WB-BC-15 is a selective c-Abl kinase inhibitor that effectively enhances radiation-induced germ-cell apoptosis. With an EC50 value of 10.5 μM, it demonstrates potential for use in cancer research, focusing on mechanisms of radio-sensitivity and apoptosis in germ cells. This compound may serve as a valuable tool for elucidating the role of c-Abl in therapeutic contexts involving radiation exposure.

Cat. No.

A33622

CAS No.

926922-16-9

AP24163

AP24163 is a selective BCR-ABL kinase inhibitor that effectively targets both wild-type BCR-ABL and the resistant variant BCR-ABL-T315I, with IC50 values of 7 nM and 511 nM, respectively. This compound serves as a valuable tool in the study of chronic myeloid leukemia (CML), enabling researchers to investigate the mechanisms of resistance and develop potential therapeutic approaches.

Cat. No.

A33623

CAS No.

2626934-64-1

c-ABL-IN-3

c-ABL-IN-3 is a potent inhibitor of the c-Abl tyrosine kinase, a target implicated in multiple diseases, particularly cancer. This compound exhibits significant biological activity that may aid in the investigation of neurodegenerative disorders such as amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) as well as various cancer types. Its utilization in research may facilitate a better understanding of c-Abl's role in disease progression and therapeutic interventions.

Cat. No.

A33624

CAS No.

305820-76-2

PD173956

PD173956 is a pyridopyrimidine compound that selectively inhibits the Bcr-Abl kinase, particularly targeting the P-loop mutant form. This inhibitor demonstrates significant activity in blocking Bcr-Abl-mediated signaling pathways, making it valuable for research on chronic myeloid leukemia and other cancers driven by Bcr-Abl mutations. Its specificity and potency support investigations into therapeutic strategies aiming to overcome resistance encountered in kinase inhibitors.

Cat. No.

A33628

CAS No.

1795736-60-5

BCR-ABL-IN-5

BCR-ABL-IN-5 is a potent Bcr-Abl kinase inhibitor that demonstrates significant inhibitory activity against both wild-type Bcr-Abl and the T315I mutant, with IC50 values of 0.014 μM and 0.45 μM, respectively. This compound exhibits anti-proliferative effects on leukemic cells, making it a valuable tool in research related to chronic myeloid leukemia and related conditions. BCR-ABL-IN-5 is suitable for studies aimed at understanding the mechanisms of Bcr-Abl-mediated oncogenesis and developing targeted therapies.

Cat. No.

A33632

CAS No.

1808287-83-3

CHMFL-ABL-053

CHMFL-ABL-053 is a potent, selective inhibitor targeting BCR-ABL, SRC, and p38 kinases, exhibiting IC50 values of 70 nM, 90 nM, and 62 nM, respectively. This compound demonstrates significant antiproliferative activity, making it a valuable tool in cancer research, particularly in studies focusing on chronic myeloid leukemia and related malignancies. Its oral bioavailability enhances its utility in in vivo research applications.