met-in-1

MET-IN-1 (Compound 13) is an orally active inhibitor of MET with antitumor activity.

c-met-IN-1 is a potent and selective c-Met inhibitor (IC50: 1.1 nM) with antitumor activity.

TAM&Met-IN-1 is a potent inhibitor of TAM and c-Met, acting on AXL (IC50: 6.1 nM), MER (IC50: 13.2 nM) and TYRO3 (IC50: 21.6 nM). TAM&Met-IN-1 can be used in anticancer studies.

VEGFR-2 c-Met-IN-1 is a dual inhibitor of VEGFR-2 and c-Met, with IC50 values of 138 nM and 74 nM, respectively, demonstrating antitumor activity [1].

PARP1 c-Met-IN-1 (Compound 16) serves as a selective dual inhibitor targeting both PARP1 and c-Met, demonstrating IC50 values of 3.3 nM and 32.2 nM, respectively. This compound effectively induces apoptosis and causes cell cycle arrest at the G2 M phase in MDA-MB-231 cells. Furthermore, PARP1 c-Met-IN-1 displays notable antitumor activity in mouse models [1].

c-Met-IN-15 exhibits antibacterial activity.

C-Met Axl-IN-1 (Compound 22a) is an oral, selective type II c-Met Axl inhibitor with IC50 values of 1 nM and 10 nM, respectively. It effectively suppresses tumor cell proliferation, induces cell cycle arrest, and apoptosis (apoptosis), showcasing potent anti-tumor activity.

c-Met-IN-12 is a selective, orally active type II c-Met kinase inhibitor (IC50: 10.6 nM). c-Met-IN-12 is a high inhibitor of AXL, Mer and TYRO3 kinases (>80% inhibition at 1 μM). c-Met-IN-12 can be used as a scaffold to further enhance kinase selectivity. c-Met-IN-12 exhibits anti-tumour activity.

c-Met-IN-16, a c-Met inhibitor, is utilized 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].

C-Met-IN-18, an ATP-competitive type-III inhibitor, targets both wild-type (WT) and D1228V mutant c-MET with IC50 values of 0.013 µM and 0.20 µM, respectively. It is utilized in research pertaining to c-MET-driven cancers [1].

c-Met-IN-17 is a potent inhibitor of c-Met kinase with an IC50 of 0.031 μM, making it relevant for anticancer research. [1]

c-Met-IN-19 (Compound 21j) is a potent c-Met inhibitor with an IC50 of 1.99 nM, demonstrating cytotoxic effects on various cancer cell lines, including A549, HT-29, SGC-7901, and MDA-MB-231, with IC50 values of 0.25, 0.36, 0.98, and 0.76 μM, respectively [1].

c-Met-IN-10 is a potent c-Met kinase inhibitor (IC50: 16 nM). c-Met-IN-10 inhibits the activity of cancer cells A549, H460 and HT-29, and inhibits A549 cell movement by inhibiting HT-29 cell colony formation, which in turn induces apoptosis in HT-29 and A549 cells. c-Met-IN-10 can be used in anticancer studies. -Met-IN-10 is capable of being used in anticancer studies.

c-Met-IN-11 is a potent inhibitor of c-MET (IC50: 41.4 nM) and VEGFR-2 (IC50: 71.1 nM).

c-Met-IN-13 is a potent inhibitor of c-Met (IC50: 2.43 nM) that exhibits significant cytotoxicity and anti-proliferative effects against cancer cells in a concentration-dependent and time-dependent manner, demonstrating therapeutic potential against cancer.

Antiproliferative Against-3 (comp 33) demonstrates significant activity against Hela (IC 50 = 0.21 µM), A549 (IC 50 = 0.39 µM), and MCF-7 (IC 50 = 0.33 µM) cell lines. Additionally, it induces apoptosis in a dose-dependent manner by arresting A549 cells in the G1 phase.

c-Met-IN-14, a N-sulfonylamidine-based derivative, is a selective c-Met kinase inhibitor with an IC50 value of 2.89 nM. It exhibits anticancer properties by inhibiting c-Met phosphorylation and arresting the cell cycle at the G2 M phase. Additionally, c-Met-IN-14 promotes dose-dependent apoptosis in A549 cells.

JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1 2 4 inhibitor (IC50: 4.7 18.7 1 nM) with over 10-fold selectivity compared to MNK2 and Fms, and no inhibition of Met, c-Kit, or PDGFRβ in the A375 cell line.

MET kinase-IN-2, a selective and potent MET kinase inhibitor, demonstrates oral bioavailability and exhibits an IC50 value of 7.4 nM. It also possesses antitumor activity[1].

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

c-Kit-IN-1 (DCC-2618) is an effective inhibitor of c-Met and c-Kit (IC50s<200 nM).

P-gb-IN-1 is a potent P-glycoprotein (P-gp) inhibitor that exhibits reverse activity by inhibiting P-gp outflow. P-gb-IN-1 has been shown to inhibit P-gp by hydrogen bonding with residues Asn 721 and Met 986. P-gb-IN-1 showed low toxicity in MCF-7 ADR cells.

Lmtk3-in-1 is a potent ATP-competitive lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM) inhibitor that degrades LMTK3 through the ubiquitin proteasome pathway. LMTK3-IN-1 has shown anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 (10-20 μM) can induce the apoptosis of BC cell line.