alk in 1

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

TRK/ALK-IN-1 is a potent dual inhibitor of TRK and ALK, exhibiting good correlation between its enzymatic inhibition and anti-proliferative activities, with IC50 values of 2.2 nM for TRKA, 9.3 nM for ALK WT, and 38 nM for ALK L1196M. It holds potential for cancer research applications.

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).

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

ALK protein ligand-1 (Compound A1) is an ALK protein ligand, acting as a ligand for the target protein in PROTACs, demonstrating inhibitory effects on ALK. It is also useful in the synthesis of AP-1.

ALK/PI3K/AKT-IN-1 (Compound 45) effectively inhibits the proliferation of cancer cell lines A549, H1975, and PC9, with IC50 values of 0.44, 0.83, and 1.51 μM, respectively. This compound enhances the expression of p21 and p27, and decreases the activity of CDK2 and p-Rb, causing cell cycle arrest at the G1 phase. It suppresses the ALK/PI3K/AKT signaling pathway, promotes mitochondrial membrane potential depolarization, and induces apoptosis in A549 cells. Furthermore, ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheres.

ALK/HDAC-IN-1 is a dual inhibitor that targets both ALK and HDAC6, demonstrating IC50 values of 16 nM and 1.03 μM, respectively. This compound exhibits anti-tumor activity.

PROTACALK degrader-1 (compound B1) is a PROTACs-based ALK degrader with a DC50 of 26 nM in H3122 EML4-ALK. It is utilized in creating PROTACALK degrader-2, which boasts excellent bioavailability.

ALK ligand-1 is an ALK ligand that can be utilized in the synthesis of PROTACALK degrader-4.

ALK/EGFR-IN-1 (Compound 8l) is a dual inhibitor targeting both ALK and EGFR, effectively blocking their phosphorylation. It demonstrates potent inhibition of ALK/EGFR mutants with IC50 values of 4.3 nM for EGFR L858R T790M in H1975 cells and 3.6 nM for EML4-ALK in BaF3 cells. This compound may be applicable in the research of non-small cell lung cancer (NSCLC) [1].

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

ALK inhibitor 1 is a selective ALK kinase inhibitor.

ALK/ROS1-IN-5 (compound X4) is a selective inhibitor of ALK and ROS1 kinases, with IC50 values of 0.512 μM for ALK and 0.766 μM for ROS1. It inhibits H2228 cells with an IC50 of 0.034 μM and induces apoptosis in cancer cells in a dose-dependent manner. Additionally, ALK/ROS1-IN-5 effectively suppresses the expression of p-ALK and p-ERK in cancer cells.

ALK/ROS1-IN-3 (compound C01) is a dual inhibitor targeting ROS1 and ALK, with IC50 values of 42.3 nM for ROS1G2032R and 49.1 nM for ALKG1202R.

ALK/ROS1-IN-4 (hydrate) (example 13) serves as a dual inhibitor of the ALK and ROS1 kinases.

PROTACEML4-ALK Degrader-2 (Pro-BA) is a selective and orally active EML4-ALK PROTAC degrader without a linker, demonstrating a DC50 of 74 nM and a T1/2 of 8 hours in H1322 cells. It relies on the GID4 and proteasome pathways to facilitate the ubiquitination of target proteins, leading to apoptosis. PROTACEML4-ALK Degrader-2 is applicable in cancer research.

ALK ligand-Linker Conjugate 1 is an ALK ligand-connector conjugate used for the synthesis of PROTACALK degrader-4.

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

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

TD-004 (HC58-111) is an innovative degrader of anaplastic lymphoma kinase (ALK) fusion proteins, effectively promoting the degradation of ALK proteins. It inhibits the growth of ALK fusion-positive cell lines SU-DHL-1 and H3122, and significantly reduces tumor growth in H3122 xenograft models.

Ensartinib (X-396) is a potent and orally active dual ALK/MET inhibitor for the treatment of ALK-positive non-small cell lung cancer (NSCLC).

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).