alk

Neladalkib (NVL-655) is a selective and brain-permeable ALK inhibitor with antitumor activity that inhibits a variety of ALK-mutant oncoproteins, and may be useful in the study of non-small cell cancers.

A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12 45 7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.

Entrectinib (RXDX-101) is a Trk, ROS1, and ALK inhibitor that inhibits TrkA, TrkB, TrkC, ROS1, and ALK (IC50=1 3 5 12 7 nM) with oral activity and blood-brain-barrier penetration. Entrectinib exhibits both antitumor and CNS activity.

Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinase inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptors.

HG-14-10-04 is a potent and specific ALK (anaplastic lymphoma kinase) inhibitor.

EML4-ALK kinase inhibitor 1 (EML4 ALK kinase inhibitor 1) is a potent oral active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.

ALK-IN-1 is a Brigatinib analog and an ALK inhibitor commonly used in anti-tumor research.

ALK inhibitor 1 is a selective ALK kinase inhibitor.

ALK-IN-26 is an ALK inhibitor with potential anticancer activity, demonstrating antiproliferative effects against glioblastoma and inducing apoptosis, autophagy, and necrosis.

ALK-IN-5 is a potent, selective, and brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 of 2.9 nM.

Crizotinib hydrochloride (PF-02341066 hydrochloride) is a novel inhibitor of anaplastic lymphoma kinase and c-Met, with IC50 values of 20 nM and 8 nM, respectively.

ALK inhibitor 2 is a new-type and selective inhibitor for the ALK kinase.

Mps1-IN-1 is a potent, selective, and ATP-competitive inhibitor of Mps1 kinase (IC50: 367 nM).

ALK-IN-6 is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK, IC50s: 71 nM, 18.72 nM, and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L).

ALK ROS1 inhibitor 2e HCL possesses anti-apoptotic, anti-proliferative and anti-tumour activities.

ALK ROS1-IN-1 is a potent and selective anti-crizotinib-resistant ALK ROS1 dual inhibitor (IC50s: 0.530 μM and 0.174 μM for ROS1 and ALK enzyme).

ALK-IN-12 is a highly potent and orally active inhibitor of anaplastic lymphoma kinase (ALK), demonstrating an exceptional IC50 value of 0.18 nM. Additionally, ALK-IN-12 displays inhibitory activity against insulin-like growth factor 1 receptor (IGF1R) and insulin receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. Notably, its antitumor effects have been observed, making it a promising compound for targeted cancer therapy.

ALK-IN-9 (compound 40) is a highly effective ALK inhibitor, demonstrating remarkable inhibitory activity against cell proliferation, with IC50 values of <0.2 nM for Ba F3-EML4-ALK, KM 12 (TPM3-TRKA), and KG-1 cell (OP2-FGFR1).

ALK ROS1-IN-4 (example 13) acts as a dual inhibitor targeting both ALK and ROS1 kinase [1].

ALK-IN-21 (Compound B10), a proficient ALK inhibitor targeting the ALKG1202R mutation, demonstrates significant inhibitory activity with IC50 values of 4.59 nM against ALK WT, 2.07 nM against ALK L1196M, and 5.95 nM against ALK G1202R. Moreover, ALK-IN-21 effectively suppresses proliferation in ALK-positive Karpas299 and H2228 cells, achieving IC50 values of 0.07 μM. It is applicable for anaplastic large cell lymphoma research [1].

ALK-IN-13 is an inhibitor of ALK (anaplastic lymphoma kinase).

ALK EGFR-IN-2 is a potent dual inhibitor targeting ALK and EGFR, promoting apoptosis and G0 G1 cell cycle arrest in cancer cells. It effectively suppresses proliferation in H1975, PC9, and Baf3-EML4-ALK cancer cell lines, with IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively [1].

SAR348830 is an ALK inhibitor, targeting anaplastic lymphoma kinase.

ALK-5-IN-1, an ALK-5 inhibitor, can be utilized for cancer research and studying conditions involving fibrosis [1].