Bcr-Abl Inhibitor

AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity. AG957 is a bcr/abl kinase inhibitor with an IC₅₀ of 2.9 μM for p210^bcr/abl autokinase activity.

AKE-72 (compound 5) is a potent inhibitor of Pan-BCR-ABL. AKE-72 inhibits BCR-ABL^WT, BCR-ABL^T315, BCR-ABL^E255K, BCR-ABL^F3171, BCR-ABL^H396P and BCR-ABL^Q252H with IC₅₀s of < 0.5, 9, 8.98, 3.12, < 1.0 and 3.88 nM, respectively. AKE-72 has anti-leukemic activity against K-562 cell line.

ON044580 is a non–ATP-competitive JAK2 and BCR-ABL kinases inhibitor. ON044580 inhibits wild-type (WT) and V617F mutant JAK2 with IC₅₀ values of 1.23 μM, 1.09 μM, respectively. ON044580 also inhibits both WT and T315I mutant BCR-ABL kinases., ON044580 blocks the IL-3–mediated phosphorylation of JAK2 and STAT5, induces apoptosis in Imatinib (HY-15463)-resistant chronic myeloid leukemia (CML). ON044580 can be used for the study of CML, myelodysplasia (MDS) and other myeloproliferative neoplasms.

Dasatinib (Standard) is the analytical standard of Dasatinib. This product is intended for research and analytical applications. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The K_is are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.

Imatinib (Standard) is the analytical standard of Imatinib. This product is intended for research and analytical applications. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.

Pro-Dasatinib (compound 2j), an amino acid analog of Dasatinib (HY-10181), is a potent Src/Abl kinase inhibitor. Pro-Dasatinib has antiproliferative activity against K652 leukemia cancer cells with an IC₅₀ of 0.21 nM.

PPY-A is a potent T315I mutant and wild-type Abl kinases inhibitor with IC₅₀s of 9 and 20 nM, respectively. PPY-A inhibits Ba?F3 cells transformed with wild-type Abl and Abl T315I mutantl with IC₅₀s of 390 and 180 nM, respectively. PPY-A can be used for the research of chronic myeloid leukemia (CML).

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

Nilotinib (Standard) is the analytical standard of Nilotinib. This product is intended for research and analytical applications. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.

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

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

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

DB07107 is a potent agent resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC₅₀ value of 360 nM.

Dasatinib (BMS-354825) (GMP) is a GMP-grade Dasatinib (HY-10181). GMP-grade small molecules can be used as adjuvant agents in cell therapy. Dasatinib (BMS-354825) is an orally active, ATP-competitive, dual Src/Bcr-Abl inhibitor with potent antitumor activity. The K_i values ​​for Src and Bcr-Abl are 16 pM and 30 pM, respectively. Dasatinib inhibits Bcr-Abl and Src with IC₅₀ values ​​of less than 1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.

Protein kinase inhibitor 6 is a protein kinase inhibitor.

PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.

Bosutinib-d₈ is a deuterium labeled Bosutinib. Bosutinib is a dual Src/Abl inhibitor with IC₅₀s of 1.2 nM and 1 nM, respectively.

Imatinib (Mesylate) (Standard) is the analytical standard of Imatinib (Mesylate). This product is intended for research and analytical applications. Imatinib Mesylate (STI571 Mesylate) is an orally active tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC₅₀=100 nM) tyrosine kinases.

BCR-ABL-IN-7 (compound 4) is a WT and T315I mutant ABL kinases inhibitor. BCR-ABL-IN-7 effectively inhibits activities of WT and T315I mutant ABL kinases. BCR-ABL-IN-7 can be used for the research of chronic myeloid leukemia (CML) research.

Ponatinib-d₈ (AP24534-d₈) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.