Bcr-Abl

Cat. No.

A24447

CAS No.

2769753-47-9

DB0614

DB0614 is a PROTAC molecule utilizing a cereblon ligand, designed as a selective and potent degrader of NEK9 and other kinases. It induces the degradation of multiple kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1–3, MAP4K5, MAPK14, MAPK7–9, MAPKAPK2/3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1/3, SIK2/3, STK35, TNK2, and ULK1. DB0614 is suitable for research involving diseases or disorders driven by aberrant kinase activity.

Cat. No.

A24736

CAS No.

2376047-73-1

SIAIS178

SIAIS178 is a potent and selective PROTAC BCR-ABL degrader that operates through the recruitment of Von Hippel-Lindau (VHL) E3 ubiquitin ligase, achieving an IC50 of 24 nM. This compound effectively induces degradation of the BCR-ABL protein, demonstrating significant anticancer activity. SIAIS178 is suitable for research applications focused on targeted protein degradation in cancer models.

Cat. No.

A24837

CAS No.

2769753-53-7

DB1113

DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions.

Cat. No.

A25131

CAS No.

2855238-97-8

VS1150

VS1150 is a BCR-ABL inhibitor that induces inhibitory phosphorylation at the Y253 site, effectively disrupting oncogenic BCR-ABL signaling with an EC50 of 69 nM. This compound not only targets the BCR-ABL fusion protein but also demonstrates inhibitory effects on other oncogenic ABL fusions and drug-resistant mutants, such as T315I. VS1150 is suitable for research applications related to chronic myeloid leukemia (CML) and other cancers driven by ABL fusions.

Cat. No.

A25841

CAS No.

552332-71-5

DB07107

DB07107 is a potent inhibitor of the T315I mutant Bcr-Abl tyrosine kinase, demonstrating resistance against this specific mutation associated with chronic myeloid leukemia. Additionally, DB07107 effectively inhibits Akt1 with an IC50 value of 360 nM, highlighting its dual-targeting capability. This compound is suitable for research applications related to cancer signaling pathways and the development of targeted therapies for resistant forms of leukemia.

Cat. No.

A30609

CAS No.

287204-45-9

PD180970

PD180970 is a potent ATP-competitive inhibitor of the p210Bcr-Abl kinase, exhibiting an IC50 of 5 nM for the inhibition of its autophosphorylation. Additionally, it inhibits Src and KIT kinases with IC50 values of 0.8 nM and 50 nM, respectively. PD180970 effectively induces apoptosis in K562 leukemic cells, making it a valuable reagent for research on chronic myelogenous leukemia.

Cat. No.

A30829

CAS No.

241127-58-2

Adaphostin

Synonyms: NSC 680410

Adaphostin, a potent inhibitor of the p210bcr/abl fusion protein (IC50 = 14 μM), exhibits significant anti-leukemic activity. It induces apoptosis in T-lymphoblastic leukemia cell lines, with IC50 values ranging from 17 to 216 nM. This compound demonstrates selective efficacy against both chronic and acute myeloid leukemia cells and increases reactive oxygen species (ROS) levels in chronic lymphocytic leukemia (CLL) B cells, making it valuable for research in leukemia therapeutics and cellular pathways related to oxidative stress.

Cat. No.

A30844

CAS No.

1258391-13-7

HG-7-85-01

HG-7-85-01 is a type II ATP competitive inhibitor that targets Bcr-Abl, including its T315I mutant, as well as PDGFRα, Kit, and Src kinases. It demonstrates potent inhibition with IC50 values of 3 nM for T315I Bcr-Abl, 20 nM for KDR, and 30 nM for RET, while showing minimal activity against other kinases (IC50 > 2 μM). HG-7-85-01 effectively inhibits cell proliferation through the induction of apoptosis and the suppression of cell-cycle progression, making it a valuable tool for research in cancer biology.

Cat. No.

A30980

CAS No.

2804039-78-7

GZD856 formic

GZD856 formic is a selective inhibitor of PDGFRα/β, displaying IC50 values of 68.6 nM and 136.6 nM, respectively, along with potent inhibition of Bcr-Abl, including the T315I mutant with IC50s of 19.9 nM and 15.4 nM. This compound exhibits notable antitumor activity, making it a valuable tool for cancer research. Additionally, GZD856 formic serves as a click chemistry reagent due to its alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating bioconjugation studies and compound labeling.

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.

A32121

CAS No.

2703834-25-5

PROTAC BCR-ABL Degrader-2

PROTAC BCR-ABL Degrader-2 is a selective degrader targeting the Bcr-AblT315 mutant, with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. This compound demonstrates a notable degradation efficacy, achieving degradation rates of 69.89% and 94.23% at concentrations of 100 nM and 300 nM, respectively. Additionally, it shows promising in vivo anti-tumor effects including significant tumor regression and induction of apoptosis in tumor cells, while maintaining a favorable safety profile. PROTAC BCR-ABL Degrader-2 is suitable for research focused on chronic myeloid leukemia (CML).

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.

A33591

CAS No.

3037776-72-7

Leu-PEG1-Dasa

Leu-PEG1-Dasa is an efficient BCR-ABL PROTAC degrader that operates through the N-terminal canonical pathway, demonstrating a DC50 of 0.48 nM. This compound utilizes a single amino acid as the E3 ligase ligand and exhibits significant anti-proliferative effects on K562 cells. Leu-PEG1-Dasa is applicable in the research of chronic myeloid leukemia (CML) and provides insights into targeted degradation mechanisms in cancer therapy.

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.

A33596

CAS No.

1268356-17-7

Nilotinib-d6

Synonyms: AMN107-d6

Nilotinib-d6 is a deuterated form of Nilotinib, a selective inhibitor of the Bcr-Abl tyrosine kinase. This compound exhibits antineoplastic activity, making it valuable in the study of chronic myeloid leukemia and other malignancies characterized by Bcr-Abl expression. Nilotinib-d6 is particularly useful in pharmacokinetic studies and metabolic profiling due to its unique isotopic labeling.

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.