multi-kinase inhibitor 1

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

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).

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].

TG 100572 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).

TG 100801 Hydrochloride is a prodrug to treat age-related macular degeneration. TG 100572 is a inhibitor of multi-targeted kinase(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src,

Amuvatinib hydrochloride (MP470 hydrochloride) is an orally administered multi-targeted tyrosine kinase inhibitor effective against mutant forms of c-Kit, PDGFRα, Flt3, c-Met, and c-Ret, and it suppresses DNA repair by inhibiting the RAD51 protein, contributing to its antineoplastic activity[1][2][3][4].

B-Raf IN 17 (Compound 8e) is an effective, orally active type II multi-kinase inhibitor. It shows potent cellular inhibition against BRAFWT, VEGFR-2, and FGFR-1 in the A375 cell line, with IC50 values of 0.02, 0.18, and 1.65 μM, respectively. B-Raf IN 17 is applicable for cancer research.

PDGFRα/β/VEGFR-2-IN-1 (6f) is a multi-targeted tyrosine kinase inhibitor that specifically targets PDGFRα, PDGFRβ, and VEGFR-2 kinases at nanomolar concentrations.

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.

Midostaurin (PKC412) is a multi-targeted tyrosine kinase inhibitor with antitumor activity, exhibiting IC50 values ranging from 22 to 500 nM against PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ, and VEGFR1/2. Midostaurin is indicated for the treatment of acute myeloid leukemia (AML) and systemic mastocytosis (SM).

Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM.

Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor that acts on KDR, Flt-1, FGFR1, and PDGFRα with IC50 values of 4 nM, 20 nM, 4 nM, and 2 nM, respectively.

Antitumor agent-70 (compound 8b) is a highly potent multi-targeted kinase inhibitor, particularly targeting c-Kit. It demonstrates remarkable anti-tumor activity and induces cell apoptosis, with strong inhibition of multiple myeloma at an IC50 value of 0.12 μM. Therefore, Antitumor agent-70 holds great potential as an effective therapy for combating cancer, especially in cases involving c-Kit. [1]

EGFR/HER2/DHFR-IN-1 is a highly selective and potent anticancer compound targeting MCF-7 breast cancer cells, acting as a multi-inhibitor for EGFR/HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. It induces cell cycle arrest at the G1/S phase and apoptosis in cells [1].

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.

Regorafenib (BAY 73-4506) mesylate is an orally active multi-target receptor tyrosine kinase inhibitor, inhibiting VEGFR1/2/3 (IC50=13/4.2/46 nM), PDGFRβ (IC50: 22 nM), Kit (IC50: 7 nM), RET (IC50: 1.5 nM), and Raf-1 (IC50: 2.5 nM), with potent anti-tumor and anti-angiogenic 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.

RGB-286638 is a multi-target CDK inhibitor that effectively hampers the kinase activity of a range of cyclin-CDK complexes, including cyclin T1-CDK9 (IC50 = 1 nM), cyclin B1-CDK1 (IC50 = 2 nM), cyclin E-CDK2 (IC50 = 3 nM), cyclin D1-CDK4 (IC50 = 4 nM), cyclin E-CDK3 (IC50 = 5 nM), and p35-CDK5 (IC50 = 5 nM). Additionally, it inhibits other kinases such as GSK-3β (IC50 = 3 nM), TAK1 (IC50 = 5 nM), Jak2 (IC50 = 50 nM), and MEK1 (IC50 = 54 nM), showcasing its versatile inhibitory potential.

O-Demethyl Lenvatinib, a metabolite of Lenvatinib (E7080), is an orally administered, multi-targeted tyrosine kinase inhibitor. It effectively inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, demonstrating significant antitumor activities [1] [2].

O-Demethyl Lenvatinib hydrochloride, a metabolite of Lenvatinib (E7080), is an orally administered multi-targeted tyrosine kinase inhibitor. It targets and inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, demonstrating potent antitumor activities [1] [2].

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].

N-Desmethyl Regorafenib N-oxide, an active metabolite of the multi-kinase inhibitor regorafenib, originates through the action of the cytochrome P450 (CYP) isoform CYP3A4. This compound demonstrates efficacy in vitro by inhibiting key enzymes such as VEGFR2, Tie2, c-Kit, and B-RAF, and it exhibits tumor growth inhibition in HT-29 and MDA-MB-231 mouse xenograft models at a dosage of 1 mg/kg.