PDGFR

PDGFR

Platelet-derived growth factor receptors (PDGFRs) belong to the receptor tyrosine kinase (RTK) family and serve the function of protein tyrosine kinases.PDGFRs are involved in a number of cellular processes, such as proliferation, migration, survival, and the emergence of cancer, and they are activated by binding to their ligand, PDGFs. Vascular endothelial cells, fibroblasts, and Kupffer cells are where PDGFRs are primarily found. The two receptor types, PDGFR- and PDGFR-, share structural similarities and are made up of intracellular kinase domains with distinctive inserts of about 100 amino acid residues that have no homology to kinases and extracellular domains with five immunoglobulin (Ig)-like domains.Direct receptor-receptor interactions involving Ig-like domain 4 stabilize the receptor dimerization, which is primarily caused by ligand binding to Ig-like domains 2 and 3.The juxtaposition of the intracellular components during dimerization, which encourages autophosphorylation in trans between the receptors, is a crucial step in activation. The phosphorylated PDGFR then recruits molecules with SH2 domains like Src kinase, Grb2, SHP2, PLC, Nck, and STAT to start various downstream signaling events.

PDGFR related products

Structure Cat No. Product Name CAS No. Product Description
V2880 AC710 1351522-04-7 AC710 is a potent, orally bioactive, and selectiveinhibitor of PDGFR (platelet-derived growth factor receptor) family kinase withKdvalues of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
V2093 AC710 Mesylate 1351522-05-8 AC710 mesylate, the mesylate salt of AC710, is a potent, orally bioactive, and selectiveinhibitor of PDGFR (platelet-derived growth factor receptor) family kinase withKdvalues of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
V0579 Amuvatinib (MP470; HPK56) 850879-09-3 Amuvatinib (MP-470; HPK-56) is a novel, potent, orally bioavailableand multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with potential antineoplastic activity.
V3285 Anlotinib 1058156-90-3 This product is discontinued due to commercial reason.Anlotinib (formerlyknown as AL3818) is a novel and potent multi-kinase inhibitor that inhibits VEGFR2/3,FGFR1-4,PDGFRα/β,c-Kit, andRet.
V3286 Anlotinib Dihydrochloride 1360460-82-7 Anlotinib Dihydrochloride (formerlyknown as AL3818 Dihydrochloride) is a novel and potent multi-kinase inhibitor that inhibits VEGFR2/3,FGFR1-4,PDGFRα/β,c-Kit, andRet.
V0577 CP-673451 343787-29-1 CP-673451 (CP673451) is a novel, potent, selective and ATP-competitive inhibitor of PDGFR(α/β) with potential antitumor activity.
V0580 Crenolanib (CP-868596; RO 002; ARO 002) 670220-88-9 Crenolanib (formerly also known as CP868596; RO-002; ARO-002), a benzimidazole compound, is an orally bioavailable and selective small molecule inhibitor of platelet-derived growth factor receptor (PDGFRα/β) with potential anticancer activity.
V79582 Gint4.T aptamer sodium Gint4.T aptamer sodium is a nuclease-resistant RNA aptamer-based antagonist targeting platelet-derived growth factor receptor beta (PDGFRβ) (Kd: 9.6 nM).
V0573 Imatinib (STI571; Gleevec; Glivec) 152459-95-5 Imatinib (formerly STI-571, trade name Gleevec and Glivec) is an orally bioavailable multi-targeted kinase inhibitor with potential anticancer activity.
V25190 INVIVO74978 778274-97-8 multikinase inhibitor 1 is a potent multikinase inhibitor.
V0576 Masitinib (AB1010) 790299-79-5 Masitinib (formerly also known as AB1010) is a novel, potent, orally bioavailable, selective and multi-targeted inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, it shows weak inhibition to ABL and c-Fms.
V29483 Methylnissolin 73340-41-7 Methylnissolin, also known as Astrapterocarpan, isolated from Astragalus membranaceus, is a novel and potent bioactive compound.
V0575 MK-2461 917879-39-1 MK-2461 (MK2461) is a novel,potent, ATP-competitive, multi-targeted inhibitor for c-Met (WT/mutants) with potential antineoplastic activity.
V69534 N-(p-Coumaroyl) Serotonin 68573-24-0 N-(p-Coumaroyl) Serotonin is a polyphenol extracted from safflower seeds that displays antioxidant, antiatherogenic, and anti-inflammatory activities.
V10056 Nintedanib esylate 656247-18-6 Nintedanib esylate (formerly also known as BIBF 1120 esylate; BIBF-1120 esylate;Vargatef), theesylate salt of nintedanib, is a novel, orally bioavailable, potent triple angiokinase inhibitor that has gained FDA approval in 2014 for the treatment of idiopathic pulmonary fibrosis (IPF).
V69531 Olaratumab (IMC-3G3; LY3012207) 1024603-93-7 Olaratumab (IMC-3G3; LY3012207) is a human monoclonal IgG1 antibody against platelet-derived growth factor receptor alpha (PDGFRα) with anti-tumor activity.
V13080 PDGF Receptor Tyrosine Kinase Inhibitor III 205254-94-0 PDGF Receptor Tyrosine Kinase Inhibitor III (also known as PDGFR Tyrosine Kinase Inhibitor III) is a novel and potent PDGFR inhibitor.
V29157 Regorafénib N-oxyde (M2) 835621-11-9 Regorafénib N-oxyde M2 is a major and active metabolite of Regorafenib.
V69536 Rinucumab (REGN 2176) 1569263-06-4 Rinucumab (REGN 2176) is a monoclonal antibody (mAb) that is an inhibitor (blocker/antagonist) of PDGF.
V3284 Ripretinib (DCC-2618) 1442472-39-0 Ripretinib (DCC-2618; DCC2618; Qinlock) is a potent, orally bioactive, and spectrum-selective pan KIT and PDGFRA inhibitor approved in 2020 as an anticancer medication for treating gastrointestinal stromalcancers.
Contact Us Back to top