mkn-45

Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent, inducing cell apoptosis and inhibiting the growth of TNBC cancer cell lines (IC50s: 10 nM - 20 nM).

AMG-337 is an effective and highly specific ATP-competitive MET kinase inhibitor. In enzymatic assays, AMG-337(AMG337) inhibits MET kinase activity (IC50: < 5 nM).

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

Atorvastatin hemicalcium salt (Atorvastatin Calcium) is an HMG-CoA reductase inhibitor with oral activity. Atorvastatin hemicalcium salt is used to lower cholesterol.

PROTACc-Met degrader-1 (Compound Met-DD4) is an orally effective PROTAC degrader targeting c-Met with a DC50 of 6.21 nM. It inhibits the proliferation of c-Met-addicted MKN-45 cells with an IC50 of 4.37 nM and causes cell cycle arrest in the G0/G1 phase. In a xenograft mouse model using MKN-45 cells, PROTACc-Met degrader-1 demonstrates antitumor activity.

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).

Antitumor Agent-90 exhibits cytotoxic effects against PC 14 and MKN 45 cells, indicating its potential utility in cancer research.

MET/PDGFRA-IN-1 (compound 8c) is an inhibitor of MET and PDGFRA proteins, with an IC50 of 36 μM against MET. It inhibits MET phosphorylation, induces apoptosis, and reduces proliferation in various MET-positive cell lines, showing IC50 values of 15.3 μM for AsPc-1, 19.0 μM for EBC-1, 22.0 μM for MKN-45, 25.6 μM for Mia-Paca-2, 21.0 μM for HT-29, and 31.5 μM for K562 [1].

MET/PDGFRA-IN-2 (compound 8h) is an inhibitor of MET and PDGFRA proteins that promotes apoptosis and impedes proliferation of MET-positive cells with IC50 values of 9.7, 6.1, 12.0, 11.5, 8.6, and 34.4 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, and K562 cells, respectively [1].