PDGFR
PDGFR (platelet-derived growth factor receptor) is a receptor tyrosine kinase family that mediates cellular responses to platelet-derived growth factors and regulates proliferation, survival, migration, and tissue development through ligand-induced receptor dimerization and autophosphorylation mechanisms[1][2]. Mechanistically, activated PDGFR recruits multiple signaling mediators, including PI3K, PLCγ, Src-family kinases, and STAT-associated pathways, thereby coordinating cell growth, differentiation, and motility programs that are essential for normal tissue homeostasis and repair[1][2]. In developmental and physiological contexts, PDGFR signaling contributes to organogenesis, mesenchymal cell function, vascular development, and tissue regeneration, highlighting its central role in multicellular tissue organization[2][3]. In disease settings, dysregulated PDGFR activity, including constitutive receptor activation and excessive ligand-driven signaling, has been associated with malignancies, gastrointestinal stromal tumors, chronic eosinophilic leukemia, and other pathological proliferative processes[1][4]. Compared with the related isoforms, PDGFRα binds PDGF-A, PDGF-B, and PDGF-C ligands, whereas PDGFRβ preferentially binds PDGF-B and PDGF-D, resulting in overlapping but biologically distinct signaling capacities and cellular responses[1]. Furthermore, PDGFRβ displays strong chemotactic signaling activity, while PDGFRα can exert different context-dependent effects on cell migration, providing a useful framework for isoform-specific experimental design[1]. For research applications, small-molecule tyrosine kinase inhibitors targeting PDGFR signaling are widely used to investigate receptor-dependent mechanisms and disease-associated signaling networks[3].
References:
- [1]. Huber M. Activation/Inhibition of mast cells by supra-optimal antigen concentrations. Cell Commun Signal. 2013 Jan 22;11(1):7. doi: 10.1186/1478-811X-11-7. PMID: 23339289; PMCID: PMC3598417. et al. Activation/Inhibition of mast cells by supra-optimal antigen concentrations. Cell Commun Signal. 2013 Jan 22;11(1):7. [Content Brief]
- [2]. Andrae J, et al. Role of platelet-derived growth factors in physiology and medicine. Genes Dev. 2008 May 15;22(10):1276-312. [Content Brief]
- [3]. Kanaan R, et al. Use of multitarget tyrosine kinase inhibitors to attenuate platelet-derived growth factor signalling in lung disease. Eur Respir Rev. 2017 Oct 25;26(146):170061. [Content Brief]
- [4]. National Library of Medicine.
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PDGFR Related Products (186)
Related Products (186)
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Linifanib (GMP)
0 ImagesCat. No.: HY-50751GCAS No.: 796967-16-3Synonyms: ABT-869 (GMP); AL-39324 (GMP)Linifanib (ABT-869) (GMP) is Linifanib (HY-50751) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Linifanib 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 (GMP) promotes the generation and reprogramming of iPSCs from somatic cells.
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UNC9750
0 ImagesCat. No.: HY-175477CAS No.: 2967648-29-7UNC9750 is an inositol phosphate multikinase (IPMK) inhibitor with IC50 values of 31.6 and 374 nM for IPMK and IP6K2, respectively.. UNC9750 inhibits cellular accumulation of InsP5, the direct product of IPMK kinase activity, while having no effect on either InsP6 or InsP7 levels. UNC9750 has ≥ 75% inhibition of four kinases (DAPK1, DYRK1B, PDGFR, and KDR). UNC9750 can be used for the study of glioblastoma.
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Multi-kinase-IN-5
0 ImagesCat. No.: HY-149415Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC50 of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively.
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PDGFRalpha T674I Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70763PDGFRalpha is a receptor tyrosine kinases that stimulate cell survival, proliferation and motility. Upon PDGF binding, the receptor dimerizes and undergoes a conformational change, which activates the kinase domain. PDGFRalpha T674I is a mutant of PDGFRalpha. PDGFRalpha T674I Recombinant Human Active Protein Kinase is a recombinant PDGFRalpha T674I protein that can be used to study PDGFRalpha T674I-related functions.
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Henatinib maleate
0 ImagesCat. No.: HY-13645ACAS No.: 1239269-52-3Henatinib maleate is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib maleate inhibits the activity of VEGFR-2, c-kit, PDGFR with IC50 values of 0.6 nM, 3.3 nM and 41.5 nM, respectively. Henatinib maleate significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway.
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Regorafénib N-oxyde-d3(M2)
0 ImagesCat. No.: HY-I0678SCAS No.: 1333489-03-4
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BOT1711
0 ImagesCat. No.: HY-P992326BOT1711 is a human IgG1κ monoclonal antibody targeting PDGFRB/CD140b. PDGFRB/CD140b belongs to type I receptor tyrosine kinases (RTKs), and is mainly expressed in vascular smooth muscle cells, pericytes, fibroblasts, certain mesenchymal stem cells, and tumor stromal cells.
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PDGFRα/FLT3-ITD-IN-3
0 ImagesCat. No.: HY-145904CAS No.: 2761259-22-5PDGFRα/FLT3-ITD-IN-3 (Compound 18d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of 0.153 and 0.004 μM, respectively. PDGFRα/FLT3-ITD-IN-3 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia.
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Lenvatinib-d5
0 ImagesCat. No.: HY-10981S1Synonyms: E7080-d5; MK-7902-d5
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Sutetinib maleate
0 ImagesCat. No.: HY-164387ACAS No.: 1701408-75-4Sutetinib maleate is the maleate form of Sutetinib (HY-164387). Sutetinib maleate is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib maleate inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo.
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KIT/PDGFRA-IN-1
0 ImagesCat. No.: HY-170911KIT/PDGFRA-IN-1 (compound 19) is a stem cell growth factor receptor (KIT) and platelet-derived growth factor receptor alpha (PDGFRA) inhibitor. KIT/PDGFRA-IN-1 inhibits KIT-wt, KIT-D816H, KIT-T670I, PDGFRA-wt, PDGFRA-D842V, PDGFRA-T674I and PDGFRA-G680R with IC50s of 2.3, 12, 492, 0.8, 99.9, 42.3, and 4.3 μM, respectively. KIT/PDGFRA-IN-1 inhibits GIST-T1, T1-a-D842V and GIST-48B cells (PDGFR- and KIT-Mutant GIST cell Lines) with GR50s of 12, 8900, ≥10 000 nM, respectively.
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Pegpleranib
0 ImagesCat. No.: HY-177655CAS No.: 1618657-13-8Synonyms: FovistaPegpleranib (Fovista) is a pegylated DNA aptamer that selectively binds to PDGF-BB and PDGF-AB homodimers and heterodimers, interrupting the interaction with their associated tyrosine kinase receptors.
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L-783277
0 ImagesCat. No.: HY-123586CAS No.: 791807-02-8L-783277 (Compound 4) is a MEK inhibitor (IC50 = 4 nM). L-783277 has potent inhibitory activity against a variety of kinases, including VEGFR2/3, FLT1/3/4, MEK1/2, KDR, and PDGFRα, but has low selectivity for the kinase community. L-783277 inhibits viability (IC50 = 22 mM) and cell proliferation (IC50 = 21 mM) of H295R cells. L-783277 could be used in research on cancers such as adrenocortical carcinoma.
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Pazopanib-13C,d3
0 ImagesCat. No.: HY-10208S1CAS No.: 1261734-88-6Synonyms: GW786034-13C,d3
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PDGFR Y1021 peptide (non-phosphorylation)
0 ImagesCat. No.: HY-P10119CAS No.: 205173-94-0
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PDGFRα kinase inhibitor 3
0 ImagesCat. No.: HY-173275PDGFRα kinase inhibitor 3 (Compound L7) is a highly potent inhibitor targeting the PDGFRαD842V kinase with IC50s values of 23.8 nM and 2.1 nM in biochemical and cellular assays, respectively. PDGFRα kinase inhibitor 3 binds to the ATP-binding pocket of PDGFRαD842V to block its downstream signaling pathways and inhibit kinase activity. PDGFRα kinase inhibitor 3 can be used for gastrointestinal stromal tumors (GISTs) study.
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PDGFRalpha D842V Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70762PDGFRalpha is a receptor tyrosine kinases that stimulate cell survival, proliferation and motility. Upon PDGF binding, the receptor dimerizes and undergoes a conformational change, which activates the kinase domain. PDGFRalpha D842V is a mutant of PDGFRalpha. PDGFRalpha D842V Recombinant Human Active Protein Kinase is a recombinant PDGFRalpha D842V protein that can be used to study PDGFRalpha D842V-related functions.
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Sunitinib-platinum(IV) prodrug-1
0 ImagesCat. No.: HY-179392Sunitinib-platinum(IV) prodrug-1 (Complex A) is a Pt(IV) prodrug based on Cisplatin (HY-17394), and this design aims to enable Pt(IV) to be reduced to active Pt(II) under intracellular reducing conditions, while simultaneously releasing a derivative of Sunitinib (HY-10255A) with tyrosine kinase inhibitor (TKI) activity. Sunitinib-platinum(IV) prodrug-1 exhibits excellent cytotoxicity against renal cell carcinoma (RCC), causing DNA crosslinking and apoptosis. Sunitinib-platinum(IV) prodrug-1 inhibits the VEGFR/PDGFR signaling pathway, suppressing tumor growth and angiogenesis. Sunitinib-platinum(IV) prodrug-1 can be used for research on renal cell carcinoma.
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Dovitinib-d8
0 ImagesCat. No.: HY-50905SCAS No.: 1246819-84-0
