Anaplastic lymphoma kinase (ALK) Inhibitor

DDO-02267 is a selective and lysine-targeting covalent inhibitor of ALKBH5, with an IC₅₀ value of 0.49 μM. DDO-02267 increases N⁶-methyladenosine (m⁶A) levels and targets the ALKBH5-AXL signaling axis. DDO-02267 can serve as a probe for investigating the biological function of mRNA demethylase.

ALK/ROS1-IN-3 (compound C01) is a ROS1 and ALK dual inhibitor with IC₅₀s of 42.3 nM and 49.1 nM for ROS1^G2032R and ALK^G1202R, respectively.

RepSox hydrochloride is a potent and selective inhibitor of transforming growth factor-β receptor I/activin-like kinase 5 (TGF-β-RI/ALK5). RepSox hydrochloride inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox hydrochloride can be used in the study of obesity and related metabolic diseases such as type 2 diabetes.

SH-CER-6 is a double-warhead C²-COUPL derived from Ceritinib (HY-187801) that targets the EML4-ALK fusion protein complex and induces its degradation. SH-CER-6 simultaneously binds to structures near the ALK inhibitor-binding region and forms a covalent conjugate with a protein cysteine, thereby promoting ubiquitination and proteasome-dependent degradation of the EML4-ALK complex, which in turn inhibits the ALK signaling pathway. SH-CER-6 is useful for research related to ALK-positive non-small cell lung cancer.

DLX-521 is an antibody that inhibits ALK. DLX-521 can be used in diagnosis and research for lung cancer.

SH-E4A-66 is a C²-COUPLr (COvalent Protein Ligator) with carbazole scaffold barring heterogeneous cysteine reactive warheads (acrylamide and chloroacetamide). SH-E4A-66 is capable of coupling with EML4-ALK (EC₅₀=1.5 μM) and inhibiting the activity of EML4-ALK kinase (IC₅₀=2.3 μM).

LY580276 is an ATP-competitive ALK5 inhibitor with an IC₅₀ of 175 nM. LY580276 inhibits transforming growth factor-β-induced epithelial-mesenchymal transition. LY580276 can be used for cancer research.

ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC₅₀s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively.

X-376 (Standard) is the analytical standard of X-376. This product is intended for research and analytical applications. X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC₅₀=0.61 nM). X-376 is a less potent inhibitor of MET (IC₅₀=0.69 nM). X-376 displays potent anti-tumor activity.

Ceritinib (Standard) is the analytical standard of Ceritinib (HY-15656). This product is intended for research and analytical applications. Ceritinib is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC₅₀ of 200 pM. Ceritinib also inhibits IGF-1R, InsR, and STK22D with IC₅₀ values of 8, 7, and 23 nM, respectively. Ceritinib shows great antitumor potency.

Ensartinib dihydrochloride (Standard) is the analytical standard of Ensartinib dihydrochloride (HY-103714A). This product is intended for research and analytical applications. Ensartinib dihydrochloride (X-396 dihydrochloride) is a BBB-permeable and dual ALK/MET inhibitor with IC₅₀s of <0.4 nM and 0.74 nM, respectively.

PF-03671148 is an ALK5 inhibitor. PF-03671148 can reduce TGFβ induced fibrotic gene expression in fibroblasts. PF-03671148 has potential utility for the prevention of dermal scarring.

5-O-Methylvisammioside (4'-O-β-D-Glucosyl-5-O-methylvisamminol) (Standard) is the analytical standard of 5-O-Methylvisammioside. This product is intended for research and analytical applications. 5-O-Methylvisammioside is an orally active natural chromone glycoside and multiple biological activities. 5-O-Methylvisammioside inhibits ferroptosis by activating the Nrf2/HO-1 signaling axis. 5-O-Methylvisammioside alleviates intestinal barrier damage by inhibiting the ROS/NF-κB/NLRP3 pathway. 5-O-Methylvisammioside exerts a protective effect against acute liver injury by reducing ALT/AST, decreasing inflammatory infiltration, and inhibiting IκB-α phosphorylation and NF-κB nuclear translocation. 5-O-Methylvisammioside blocks the HMGB1/RAGE/MEK/ERK signaling axis to exert anti-tumor and anti-angiogenic effects. 5-O-Methylvisammioside improves depression-like behaviors by inhibiting Src kinase and the NF-κB pathway.

Repotrectinib (Standard) is the analytical standard of Repotrectinib (HY-103022). This product is intended for research and analytical applications. Repotrectinib (TPX-0005) is a potent ROS1 (IC₅₀=0.07 nM) and TRK (IC₅₀=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC₅₀=1.01 nM). Repotrectinib has anti-cancer activity.

CEP-14083 is a ATP-competitive ALK kinase inhibitor with an IC₅₀ value in enzymatic assays of 2 nM. CEP-14083 also inhibits other kinases, such as insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2) and dual leucine zipper kinase (DLK). CEP-14083 suppresses CD274 mRNA expression and the NPM/ALK function in the NPM/ALK-carrying T cell lymphoma (ALK+TCL) cells. CEP-14083 is promising for research of lymphoma.

NVP-TAE 684 (Standard) is the analytical standard of NVP-TAE 684 (HY-10192). This product is intended for research and analytical applications. NVP-TAE 684 (TAE 684) is a highly potent and selective ALK inhibitor, which blocks the growth of ALCL-derived and ALK-dependent cell lines with IC₅₀ values between 2 and 10 nM.

ALK/ROS1-IN-4 (hydrate) (example 13) is a dual inhibitor of ALK and ROS1 kinase.

Brigatinib (Standard) is the analytical standard of Brigatinib. This product is intended for research and analytical applications. Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC50 of 0.6 nM. Brigatinib can be used for research of NSCLC.

EML4-ALK K_inase inhibitor 1 (Standard) is the analytical standard of EML4-ALK K_inase inhibitor 1 (HY-111752). This product is intended for research and analytical applications. EML4-ALK K_inase inhibitor 1 is a potent orally active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma K_inase (EML4-ALK), with an IC₅₀ of 1 nM.

Crizotinib-d₈ (PF-02341066-d₈) is deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.