Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation[1][2][3][4].
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively.
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 2.1 nM/3.2 nM, 0.74 nM, respectively.
Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases[1].
Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
AG 370, an indole tyrphostin, is a potent PDGF-induced mitogenesis inhibotor (IC50 of 20 μM). AG 370 displays weak inhibition of the EGF receptor[1].
Multi-kinase-IN-1 (Compound 11k) is a potent kinase inhibitor with antitumor activity. Multi-kinase-IN-1 induces cell apoptosis, and can be studied for colorectal cancer[1].
Rinucumab (REGN 2176), a monoclonal antibody, is a PDGF inhibitor. Rinucumab (REGN 2176) could be used for the study of neovascular age-related macular degeneration[1].
Toceranib-d8 (SU11654-d8) is the deuterium labeled Toceranib. Toceranib (SU11654) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib (SU11654) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors[1][2].
JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM)[1][2].
PDGFRα/FLT3-ITD-IN-1 (Compound 12d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 0.036 and 0.003 μM, respectively. PDGFRα/FLT3-ITD-IN-1 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia[1].
SU4312 is the racemate of (Z)-SU4312 and (E)-SU4312. (Z)-SU4312 inhibits PDGFR and FLK-1 with IC50s of 19.4 and 0.8 μM, respectively. (E)-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively[1].
N-(p-Coumaroyl) Serotonin is a polyphenol isolated from the seeds of safflower and has antioxidative, anti-atherogenic and anti-inflammatory properties. N-(p-Coumaroyl) Serotonin inhibits PDGF-induced on phosphorylation of PDGF receptor and Ca2+ release from sarcoplasmic reticulum[1]. N-(p-Coumaroyl) Serotonin ameliorates atherosclerosis and distensibility of the aortic wall in vivo and is usually used for the atherosclerosis research[2].
PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively[1].
Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity[1][2][3].
PDGFRα/FLT3-ITD-IN-2 (Compound 13d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 20 and 1.654 μM, respectively. PDGFRα/FLT3-ITD-IN-2 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia[1].
Pazopanib-13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride[1]. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].
PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma[1].
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].