multikinase

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

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 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-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 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.

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].

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

SKLB 1028 (Ruserontinib) is a new type of oral multikinase inhibitor of EGFR, FLT3, and Abl. SKLB 1028 shows excellent activity in FLT3-driven AML models and considerable potency in CML models containing Abl mutants.

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity

Sorafenib D4 is the deuterium labeled Sorafenib. Sorafenib is an inhibitor of multikinase (Raf-1, B-Raf, and VEGFR-3 IC50s of 6 nM, 20 nM, and 22 nM, respectively).

Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively).

Donafenib (Bay 43-9006 (D3)) is a deuterium-labeled Sorafenib which is a multikinase inhibitor(IC50s: 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively).

PT109 is a multikinase inhibitor that targets JNK and other kinases, playing a crucial role in anti-inflammatory, antioxidative, neurogenic, and synaptogenic processes. Specifically, PT109 inhibits JNK isoforms with the following IC50 values: JNK1 at 0.143 μM, JNK2 at 0.831 μM, and JNK3 at 0.285 μM. It also inhibits SGK isoforms (SGK1: IC50=1.34 μM; SGK2: IC50=5.6 μM; SGK3: IC50=26.4 μM) and ROCK2 (IC50=34 μM). Additionally, PT109 reprograms polymorphic glioblastoma multiforme (GBM) into oligodendroglia via the PTBP1/PKM1/2 pathway and alters the metabolic pattern of GBM to exhibit antiglioma activity.

VEGFR-2-IN-5 (UNC0064-12), multikinase inhibitor and has a -NH2 terminal linker for further synthesis.

UNC9750 is an inhibitor of inositol phosphate multikinase (IPMK), with IC50 values of 31.6 nM for IPMK and 374 nM for IP6K2. It effectively suppresses the accumulation of InsP5, a direct product of IPMK kinase activity, without affecting InsP6 or InsP7 levels. Additionally, UNC9750 inhibits over 75% of the activity of four kinases: DAPK1, DYRK1B, PDGFR, and KDR. This compound is applicable in glioblastoma research.

Tinengotinib is a multikinase inhibitor targeting a series of kinases involved in cancer cell proliferation, angiogenesis, and regulation of immune response, including Aurora kinase A/B, Janus kinase (JAK1/2), fibroblast growth factor receptor (FGFR1/2/3), vascular endothelial growth factor receptors (VEGFRs), and other tyrosine kinases. Tinengotinib has shown good tolerability and preliminary efficacy in clinical trials in a variety of advanced solid tumors.

AD80, a multikinase inhibitor, targets RET, RAF, SRC, and S6K with significantly reduced activity on mTOR.

PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III) is a multikinase inhibitor that inhibits PDGFR, EGFR, FGFR, PKA, and PKC and can be used for research on amyotrophic lateral sclerosis [1].