multi-kinase

Multi-kinase inhibitor 1 (Multi-kinase inhibitor I) is a Multi-kinase inhibitor.

Multi-kinase inhibitor 3 (compound 12) is an orally active and effective multikinase (multikinase) inhibitor, demonstrating potent IC50 values against FLT1/VEGFR1, KDR/VEGFR2, FLT4/VEGFR3, FLT3, PDGFRα, and PDGFRβ, at 1.59, 1.23, 1.19, 0.59, 0.22, and 1.15 nM respectively. This compound exhibits anti-proliferative and anticancer activities.

Multi-kinase inhibitor 4 (compound 14) serves as an orally effective inhibitor targeting FLT1, KDR, FLT3, FLT4, PDGFRα, and PDGFRβ, exhibiting IC50 values of 1.97 nM, 1.04 nM, 0.33 nM, 1.44 nM, 0.18 nM, and 0.89 nM respectively. This compound plays a crucial role in cancer research.

4SC-203 is a multi-kinase inhibitor with potential anti-tumor activity. 4SC-203 exhibits unique selectivity for Flt3, Flt3 mutants, Axl, Alk, Fak, VEGF-R2, and Trk receptors in the low nM range.

Multi-kinase-IN-5 (compound 15c) is a multi-kinase inhibitory agent that demonstrates significant inhibition of a range of protein kinases, including RET (69%), KIT (31%), cMet (62%), VEGFR1 (40%), VEGFR2 (73%), FGFR1 (74%), PDGFR (59%), and BRAF (74%). Its IC50 values are 1.287 μM for FGFR1, 0.117 μM for VEGFR, and 1.185 μM for RET kinases, indicating its potency [1].

Multi-kinase-IN-7 is a multi-kinase inhibitor with IC50 values of 2.19, 2.95, 3.59, and 9.31 μM against EGFR, VEGFR2, TrKA, and CDK2, respectively. It demonstrates moderate to weak activity on FAK, AKT1, GSK3β, and CDK5, with IC50 values of 6.3, 9.2, 11.7, and 23.4 μM, respectively. Multi-kinase-IN-7 exhibits broad-spectrum antiproliferative potential against NCI cancer cell lines and can induce cell cycle arrest, apoptosis (apoptosis), and necrosis. MDA-MB-231 is applicable in breast cancer research.

Multi-kinase-IN-8 is a multi-kinase inhibitor. It effectively inhibits COX-1 (IC50 = 12.6 μM), COX-2 (IC50 = 0.05 μM), and VEGFR-2 (IC50 = 0.12 nM). Additionally, it blocks tumor-associated carbonic anhydrases CA IX and CA XII with Ki values of 31.5 nM and 386.9 nM, respectively, and induces cell cycle arrest and apoptosis (apoptosis) by upregulating Caspase-9 and Bax, while downregulating Bcl-2. Multi-kinase-IN-8 also suppresses the expression of PGE2, p-VEGFR-2, MMP-9, and HIF-1α, and demonstrates growth inhibitory activity on breast, lung, and colorectal adenocarcinomas.

Multi-kinase-IN-10 (Compound IIIk) is a multi-kinase inhibitor with notable calcium channel blocking activity, exhibiting an IC50 of 26.67 μM. It acts as a potent dual cholinesterase inhibitor, with IC50 values of 0.304 μM for hAChE and 1.033 μM for hBuChE. Additionally, Multi-kinase-IN-10 demonstrates antioxidant and neuroprotective properties, along with significant anti-amnesic activity, making it suitable for Alzheimer's disease research.

Multi-kinase-IN-3 (compound 2) is a potent angiokinase inhibitor, targeting VEGFR-2 with an IC50 of 58.3 nM and PDGFRβ with an IC50 of 55 nM.

Multi-kinase-IN-2 is an orally active inhibitor of angiokinases. multi-kinase-IN-2 significantly inhibits the activity of angiokinases such as VEGFR-1/2/3, PDGFRα/β, FGFR-1, LYN and c-KIT kinases. -IN-2 significantly attenuates phosphorylation of AKT and ERK proteins, induces apoptosis and has anticancer effects.

Multi-kinase-IN-1, a powerful kinase inhibitor, exhibits antitumor properties by inducing cell apoptosis. It is under investigation for its potential application in treating colorectal cancer.

Multi-kinase-IN-4 (compound 5d) is a multi-targeted kinase inhibitor effective against VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18, and 2.09 μM, respectively. It shows broad-spectrum anti-cancer activity in HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50: 1.94–7.1 µM) and exhibits lower toxicity in WI-38 cells (IC50 = 40.85 µM). Additionally, it induces apoptosis, causes S-phase cell cycle arrest in HepG2 cells, and holds potential for cancer research [1].

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that impedes the activity of TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. It exhibits antiproliferative effects on MCF7, HCT116, and EKVX cancer cell lines with IC50s of 3.36 μM, 1.40 μM, and 3.49 μM, respectively. Additionally, Multi-kinase-IN-6 induces cell cycle arrest at the G1/S and G1 phases in MCF7 and HCT116 cells, respectively, and effectively triggers apoptosis [1].

Multi kinase ligand 4 is a target protein ligand utilized in the synthesis of PROTACDB-0646.

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.

Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4/20/0.4/2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma.

Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).

Tesevatinib (XL-647) is an oral, multi-targeted tyrosine kinase inhibitor with IC50 values ​​of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4.

TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2].

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.

Genistein (NPI 031L) is a naturally occurring soy isoflavone, a multi-targeted tyrosine kinase inhibitor. Genistein has antitumor, antioxidant, and anthelmintic properties, and also produces estrogen-like effects in the body.

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.