yingweiwo

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
AC 710 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.
AC710 Mesylate 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.
cis-SU4312 V88059 cis-SU4312 90828-16-3 cis-SU4312 ((Z)-SU4312) inhibits PDGFR and FLK-1 with IC50 of 19.4 and 0.8 μM, respectively.
CP 673451 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.
Gint4.T aptamer sodium 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).
INVIVO74978 V25190 INVIVO74978 778274-97-8 multikinase inhibitor 1 is a potent multikinase inhibitor.
MK-2461 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.
N-(p-Coumaroyl) Serotonin 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.
PDGF Receptor Tyrosine Kinase Inhibitor III 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.
PDGFRα/β/VEGFR-2-IN-1 V88058 PDGFRα/β/VEGFR-2-IN-1 PDGFRα/β/VEGFR-2-IN-1 (6f) is a multiple PDGFRα/β and VEGFR-2 tyrosine kinase inhibitor that specifically targets PDGFRα, PDGFRβ, and VEGFR-2 kinases at nanomolar concentrations.
Seralutinib (PK-10571; GB-002) V41775 Seralutinib (PK-10571; GB-002) 1619931-27-9 Seralutinib (PK-10571; GB-002) is a novel and potent PDGFRα/β inhibitor used as an inhaled formulation for the treatment of PAH (pulmonary arterial hypertension).
SU-4312 V15397 SU-4312 5812-07-7 SU-4312, formerly known as DMBI, is a potent and selective inhibitor of VEGFR and PDGFR tyrosine kinases (IC50 are 0.8 and 19.4 μM respectively).
SU14813 maleate V29102 SU14813 maleate 849643-15-8 SU14813 maleate is a novel, orally bioavailable, multi-targeted tyrosine kinase inhibitor (TKI) with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT, respectively.
TAK-593 V4585 TAK-593 1005780-62-0 TAK-593 is a novel, orally bioavailable and potent small-molecule receptor of VEGFR and PDGFR with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
Toceranib-d8 (Toceranib d8) V69297 Toceranib-d8 (Toceranib d8) 1795134-78-9 Toceranib-d8 is the deuterated form of Toceranib.
Tyrphostin AG 1296 V0574 Tyrphostin AG 1296 146535-11-7 Tyrphostin AG 1296 (AG-1296) is a novel, potent, selective and ATP-competitive inhibitor of PDGFR with potential antitumor activity.
伊马替尼 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.
克莱拉尼 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.
妥拉尼布 V3698 Toceranib 356068-94-5 Toceranib (formerly known as PHA-291639, or SU-11654) is an inhibitor of receptor tyrosine kinase (RTK) with anticancer activities.
安罗替尼 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.
Contact Us