Anaplastic lymphoma kinase (ALK) Inhibitor

Kaempferol 3-O-gentiobioside is an orally active flavonoid, with a K_a value of 57 µM against human NOTCH1 and an IC₅₀ value of 50 μM against α-glucosidase. Kaempferol 3-O-gentiobioside inhibits the NOTCH signaling pathway. It downregulates the expression of TLR4 and NLRP3, and suppresses the activation and nuclear translocation of NF-κB. Kaempferol 3-O-gentiobioside inhibits the expression of MUC5AC, reduces nitrite and ROS levels, and attenuates excessive mucus secretion. It exhibits antibacterial activity, reducing the formation and growth of MRSA biofilms. Kaempferol 3-O-gentiobioside blocks the TGF-β/ALK5/Smad signaling pathway and inhibits epithelial-mesenchymal transition. It suppresses the proliferation, migration, invasion and metastatic growth of tumor cells. Kaempferol 3-O-gentiobioside alleviates airway inflammation and mucus hypersecretion in mice with allergic asthma. It reduces the volume of ovarian cancer xenografts in mice. Kaempferol 3-O-gentiobioside can be used in research related to allergic asthma, diabetes, MRSA infection, breast cancer, gastric cancer and ovarian cancer.

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.

MS4077 is an ALK PROTAC degrader with a DC₅₀ of 3 nM in SU-DHL-1 cells, a DC₅₀ of 34 nM in NCI-H2228 cells, and a K_d of 37 nM. MS4077 induces the degradation of oncogenic active ALK fusion proteins via a cereblon- and proteasome-dependent pathway, and inhibits the phosphorylation of ALK and STAT3, thereby suppressing cancer cell proliferation. MS4077 is used for the research of anaplastic large cell lymphoma and non-small cell lung cancer.

Brigatinib C is a prodrug of ALK inhibitor, which can be used to syntheis PROTACs.

Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has K_is of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK^L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC₅₀s of 15-43 nM (ALK^L1196), 14-80 nM (ALK^G1269A), 38-50 nM (ALK^1151Tins), 77-113 nM (ALK^G1202R), respectively.

ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC₅₀ value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research.

TGF-βRI inhibitor 3 (Compound 9ac) is a selective TGF-β inhibitor. TGF-βRI inhibitor 3 can effectively inhibit the TGF-β signaling pathway. TGF-βRI inhibitor 3 has IC₅₀ values of 13 μM and 0.63 μM for c-Src kinase and ALK5 kinase, respectively.

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice.

Itacnosertib hydrochloride (TP-0184 hydrochloride) is the inhibitor for FLT3, ACVR1 (ALK2, IC₅₀=8 nM) and JAK2 (IC₅₀=8540 nM). Itacnosertib hydrochloride exhibits anti-leukemic activity.

Crizotinib-d₅ is the 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.

Ena15 is an ALKBH5 inhibitor. Ena15 enhances the demethylase activity of FTO. Ena15 increases m⁶A RNA level, and stabilizes FOXM1 mRNA. Ena15 suppresses the growth activity of glioblastoma multiforme.

JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC₅₀ of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.

Ficonalkib is a potent inhibitor of Anaplastic lymphoma kinase (ALK), the tyrosine kinase receptor. Ficonalkib, can be used as an antineoplastic agent.

ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC₅₀=37 nM) and focal adhesion kinase (FAK; IC₅₀=5 nM).

ALK-IN-28 (compound 22) is an inhibitor of anaplastic lymphoma kinase (ALK).

ALK kinase inhibitor-1 is an anaplastic lymphoma kinase (ALK) inhibitor extracted from patent US20130261106A1 compound I-202.

XMU-MP-5 is a selective inhibitor for ALK. XMU-MP-5 inhibits ALK-mutated Ba/F3 cell with IC₅₀s of 4-50 nM, and induces apoptosis in EML4-ALK Ba/F3. XMU-MP-5 exhibits antitumor efficacy in mice.

KRCA-0008 is a selective ALK/Ack1 inhibitor with IC₅₀s of 12 and 4 nM for ALK and Ack1, respectively. KRCA-0008 can be used for the research of cancer.

6-Demethoxytangeretin is a flavonoid compound that can be isolated from Citrus reticulata. 6-Demethoxytangeretin has anti-inflammatory and anti-allergic activities and can inhibit the production of IL-6 and the expression of related genes in human mast cells through the ALK and MAPK pathways. 6-Demethoxytangeretin can promote CRE-mediated transcription in hippocampal neurons.

HG-14-10-04 is a potent ALK and mutant EGFR inhibitor with IC₅₀s of 20 nM, 15.6 nM, 22.6 nM and 124.5 nM for ALK, EGFR^LR/TM, EGFR^19del/TM/CS and EGFR^LR/TM/CS, respectively. HG-14-10-04 can be used to research anticancer.