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Bcr-Abl inhibitors target the constitutively active fusion tyrosine kinase encoded by the Philadelphia chromosome. The translocation joins the breakpoint cluster region (BCR) gene to the Abelson tyrosine kinase gene (ABL1) on chromosome 22. Expression of the P210 form of Bcr-Abl in mouse bone marrow cells induced a disease resembling chronic myelogenous leukemia (CML) in 1990. In 1996 imatinib (CGP 57148), listed here as the base and as imatinib mesylate, was reported to inhibit Abl and Bcr-Abl-positive cell growth. Dasatinib, described in 2004, also inhibits Src family kinases and blocks many imatinib-resistant Abl mutants. Nilotinib and bafetinib are further Abl inhibitors, and ponatinib also inhibits the T315I gatekeeper mutant.
Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 a and VEGF in U266 cell line in a time- and dose-dependent manners, so flumatinib mesylate may become a new drug for MM therapy.
Synonyms: AN019
NRC-AN-019 is an orally administered tyrosine kinase inhibitor (TKI) of the Bcr-Abl protein-tyrosine kinase. NRC-AN-019 is more effective in inhibiting angiogenic potential and proliferation of both MDAMB231 and HTB20/BT474 cells.
Synonyms: NVP-AST 487
AST487 is a Ret kinase inhibitor/FLT3 inhibitor with IC50 of 0.88 uM for Ret.
Synonyms: GZD-824 Dimesylate; GZD824
GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.
GNF-7 is a potent type-II kinase Bcr-Abl inhibitor with IC50 of
Synonyms: HHGV678
Flumatinib is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRbeta and c-Kit respectively.
Synonyms: GZD 824
GZD824 is a novel orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including T315I.
Synonyms: INNO406; NS187; Bafetinib
Lyn-IN-1 is a potent and selective dual Bcr-Abl/Lyn inhibitor, extracted from patent WO2014169128A1.
ON 146040 is the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways; inhibits PI3K α/δ isoforms with IC50 of 14/20 nM.
Synonyms: AMN107 hydrochloride
Nilotinib hydrochloride is a potent Bcr-Abl tyrosine kinase inhibitor that exhibits significant antineoplastic activity. It is primarily utilized in research related to chronic myelogenous leukemia (CML), providing valuable insights into the molecular mechanisms of this disease and potential therapeutic strategies. Its oral bioavailability makes it a convenient choice for in vitro and in vivo studies focused on targeting the Bcr-Abl fusion protein.
CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively.
Synonyms: CZC-00008004
CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase.
AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.
SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5μM.
Synonyms: ABL001
Asciminib (ABL001) is a potent and selective allosteric Bcr-Abl inhibitor; inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
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.
BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.
Synonyms: 1-NA-PP 1 hydrochloride
1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).
Synonyms: K-0706
Vodobatinib, also known as K-0706, is a novel 3rd generation (3G) TKI effective against wild-type and mutated BCR-ABL1 with limited off-target activity.
Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.
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.
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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.
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.
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.
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.
