Bcr-Abl Inhibitor

CHMFL-ABL-053 (Compound 18a) is a potent, selective, and orally available BCR-ABL, SRC and p38 kinase inhibitor with IC₅₀ values of 70, 90 and 62 nM against ABL1, SRC and p38, respectively.

DosatiLink-2 is an Abelson murine leukemia (ABL) enzyme inhibitor.

BCR-ABL-IN-13 is a dual c-Src and Abl inhibitor, with a K_i value of 0.55 μM against c-Src, 0.10 μM against wild-type Abl, and 0.40 μM against the Abl^T315I mutant. BCR-ABL-IN-13 exerts competitive/mixed-type inhibitory effects on wild-type Abl, and non-competitive inhibitory effects on the drug-resistant Abl^T315I mutant. BCR-ABL-IN-13 can be used for the research of chronic myeloid leukemia.

EGFR-IN-216 is an epidermal growth factor receptor (EGFR) tyrosine kinase (TK) inhibitor. EGFR-IN-216 inhibits EGFR tyrosine kinase phosphorylation, blocks downstream signaling pathway activation, suppresses cancer cell proliferation and promotes tumor cell apoptosis (apoptosis). EGFR-IN-216 can be used for the research of non-small cell lung cancer.

CpCDPK1/TgCDPK1-IN-1 (compound 7p) is a potent CpCDPK1/TgCDPK1 dual inhibitor (IC₅₀: 10 nM and 5.0 nM respectively). CpCDPK1/TgCDPK1-IN-1 also inhibits Abl and Src (IC₅₀: 75 nM and 65 nM respectively). CpCDPK1/TgCDPK1-IN-1 can be used for research of toxoplasmosis.

cSRC/BCR-ABL1-IN-1 (compund 16a) is a dual-target cSRC/BCR-ABL1 kinase inhibitor.

Kinase modulator-1 (P142, MS: m/z445) is a kinase modulator. Kinase modulator-1 can inhibit Bcr-Abl activity, especially against drug-resistant mutant kinases (such as T315I Bcr-Abl). Kinase modulator-1 can be used for cancers like chronic myelogenous leukemia (CML) research.

Tyrosine kinase-IN-12 is a selective kinase inhibitor with inhibitory activity against human tyrosine kinases KDR, Abl, Lyn and Fyn.

Bosutinib (Standard) (SKI-606 (Standard)) hydrate is the analytical standard of Bosutinib hydrate (HY-10158A). This product is intended for research and analytical applications. Bosutinib hydrate is an oraly activel Src/Abl tyrosine kinase inhibito with IC₅₀s of 1.2 nM and 1 nM, respectively.

Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI). Tyrosine kinase-IN-8 shows anti-proliferative activity against K562 cells, a chronic myeloid leukemia (CML) cell line (CC₅₀=0.8 µM). Tyrosine kinase-IN-8 can be used in the study of chronic leukemia.

VS1150 (Compound 11) is a BCR-ABL-targeting phosphorylation-inducing chimeric small molecule (PHICS). VS1150 significantly inhibits oncogenic kinase BCR-ABL signaling by inducing inhibitory phosphorylation at its Y253 (EC₅₀: 69 nM), subsequently triggering cell apoptosis. VS1150 also inhibits other oncogenic ABL fusions and drug-resistant mutants like T315I. VS1150 can be used for chronic myeloid leukemia (CML) and other ABL fusion-driven cancers research.

KW-2478 hydrochloride is an HSP90 inhibitor (IC₅₀ = 3.8 nM). KW-2478 hydrochloride inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 hydrochloride weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 hydrochloride downregulates STAT3 expression. KW-2478 hydrochloride may be used in research on cancers such as CML and liver cancer.

BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC₅₀ of 6.46, and may be used in the research of chronic myelogenous leukemia.

BCR-ABL-IN-9 (Compound B1) is a BCR-ABL inhibitor that achieves sustained BCR-ABL suppression by forming stable covalent bonds with the ABL kinase. BCR-ABL-IN-9 is also effective in inhibiting the activity of the ABL kinase (IC₅₀ = 1.2 nM). BCR-ABL-IN-9 possesses anticancer activity.

Meribatinib (compound 17) is a potent allosteric inhibitor of Bcr-Abl kinase. Meribatinib binds to the myristoyl binding pocket of the Bcr-Abl protein, locking the kinase domain in an inactive state. Meribatinib can be used for research on chronic myeloid leukemia.

ML786 is a potent and orally bioavailable Raf inhibitor, with IC₅₀s of 2.1, 4.2, and 2.5 nM for ^V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC₅₀=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 can be used for the research of cancers.

BCR-ABL-IN-14 is a tyrosine kinase inhibitor targeting BCR-ABL1, ABL1 and ABL2. BCR-ABL-IN-14 inhibits chronic myeloid leukemia cells. It is applicable to research related to chronic myeloid leukemia, acute myeloid leukemia and acute lymphoblastic leukemia.

(S)-Embibatinib ((S)-TERN-701), an isomer of TERN-701 (HY-182792), is a selective BCR-ABL allosteric inhibitor. (S)-Embibatinib can be usd for the research of cancer.

c-ABL-IN-2 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-2 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2020260871A1, compound 25). c-ABL-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

BCR-ABL-IN-6 (9h) is a selective Bcr-Abl kinase inhibitor with IC₅₀s of 4.6 and 227 nM for Bcr-Abl^WT and Bcr-Abl^T3151 respectively. BCR-ABL-IN-6 inhibits Bcr-Abl kinase with strong affinity inside the cells with an EC₅₀ of 14.6 nM. BCR-ABL-IN-6 is an imatinib derivative which can be used for research of chronic myelogenous leukemia. BCR-ABL-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.