PDGFR

Ponatinib (AP24534) (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

A multi-kinase inhibitor

inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase

A multi-kinase inhibitor

SU 5402 is a multi-targeted receptor tyrosine kinase inhibitor that inhibit against vascular endothelial growth factor receptor 2 (VEGF-R2) and fibroblast growth factor receptor 1 (FGF-R1) tyrosine kinase activity with IC 50 values of 20 and 30nM, respectively.

Pacritinib (SB1518) (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib (SB1518) also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).

A dual VEGFR and PDGFR family kinase inhibitor

Crenolanib (CP-868596) 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 0.74 nM and 2.1 nM/3.2 nM, respectively.

Tandutinib (MLN518) (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib (MLN518) can be used for acute myelogenous leukemia (AML). Tandutinib (MLN518) has the ability to cross the blood-brain barrier.

V-Abl/c-Kit/PDGFR inhibitor

E7080, known as lenvatinib, is an oral multitargeted tyrosine kinase inhibitor including VEGF, FGF and SCF receptors that has been shown to improve the survival rate of patients with radioiodine-refractory thyroid cancer.

Chk1 inhibitor,novel and potent

potent and selective inhibitor of PDGF receptor kinase

A multi-kinase inhibitor

A multi-targeted RTK inhibitor

Cediranib (AZD217) (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

A multi-kinase inhibitor

TSU-68 (SU6668,Orantinib) (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.

PDGFRβ inhibitor

Sorafenib acts as a multi-kinase inhibitor, targeting Raf-1 and B-Raf with IC 50 values of 6 nM and 22 nM, respectively.

Linifanib (ABT-869) (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib (ABT-869) shows prominent antitumor activity. Linifanib (ABT-869) has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib (ABT-869) is a specific miR-10b inhibitor that blocks miR-10b biogenesis.

inhibitor of VEGFR-2, PDGFRβ, Flt-3, and c-Kit

Avapritinib is a potent and selective exon 17 mutant KIT kinase inhibitor with IC50 of 0.27 nM for KIT D816V.

Trapidil (AR-12008) is a vasodilator, is an antiplatelet drug with specific platelet-derived growth factor.