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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Multi-kinase inhibitor 1 (Standard)
0 ImagesCat. No.: HY-103032RCAS No.: 778274-97-8Multi-kinase inhibitor 1 (Standard) is the analytical standard of Multi-kinase inhibitor 1 (HY-103032). This product is intended for research and analytical applications. Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.
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Dovitinib lactate (Standard)
0 ImagesSynonyms: CHIR-258 lactate (Standard); TKI-258 lactate (Standard)Dovitinib (lactate) (Standard) is the analytical standard of Dovitinib (lactate). This product is intended for research and analytical applications. Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
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Lenvatinib mesylate (Standard)
0 ImagesSynonyms: E7080 mesylate (Standard)Lenvatinib (mesylate) (Standard) is the analytical standard of Lenvatinib (mesylate). This product is intended for research and analytical applications. 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.
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Pazopanib-d3 hydrochloride
0 ImagesCat. No.: HY-W705479CAS No.: 2469755-67-5Synonyms: GW786034-d3 hydrochloridePazopanib-d3 (hydrochloride) (GW786034-d3 (hydrochloride)) is deuterium labeled Pazopanib (Hydrochloride). 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.
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AG 1295 (Standard)
0 ImagesAG 1295 (Standard) is the analytical standard of AG 1295. This product is intended for research and analytical applications. AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor.
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Vorolanib (Standard)
0 ImagesCat. No.: HY-109019RCAS No.: 1013920-15-4Synonyms: CM082 (Standard); X-82 (Standard)Vorolanib (Standard) is the analytical standard of Vorolanib (HY-109019). This product is intended for research and analytical applications. Vorolanib (CM082) is an orally active, potent multiKinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
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ENMD-2076 (Standard)
0 ImagesCat. No.: HY-10987ARCAS No.: 934353-76-1ENMD-2076 (Standard) is the analytical standard of ENMD-2076 (HY-10987A). This product is intended for research and analytical applications. ENMD-2076 is a multi-targeted Kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KdR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
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SU 5402 (Standard)
0 ImagesCat. No.: HY-10407RCAS No.: 215543-92-3
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Ripretinib (Standard)
0 ImagesSynonyms: DCC-2618 (Standard)Ripretinib (Standard) is the analytical standard of Ripretinib. This product is intended for research and analytical applications. Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2). DCC-2618 exerts antineoplastic effect and induces apoptosis.
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Regorafenib Hydrochloride (Standard)
0 ImagesSynonyms: BAY 73-4506 hydrochloride (Standard)Regorafenib (Hydrochloride) (Standard) is the analytical standard of Regorafenib (Hydrochloride). This product is intended for research and analytical applications. Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
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Quizartinib (Standard)
0 ImagesSynonyms: AC220 (Standard)Quizartinib (AC220) (Standard) is the analytical standard of Quizartinib (HY-13001). This product is intended for research and analytical applications. Quizartinib is an orally active, potent and selective FLT3 inhibitor. Quizartinib inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib can be used for the research of cancer.
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Tandutinib sulfate
0 ImagesCat. No.: HY-10202BCAS No.: 387867-14-3Tandutinib (MLN518) sulfate 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 sulfate can be used for acute myelogenous leukemia (AML). Tandutinib sulfate has the ability to cross the blood-brain barrier.
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Ponatinib (Standard)
0 ImagesSynonyms: AP24534 (Standard)Ponatinib (Standard) is the analytical standard of Ponatinib. This product is intended for research and analytical applications. Ponatinib (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.
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Ponatinib hydrochloride (Standard)
0 ImagesSynonyms: AP24534 hydrochloride (Standard)Ponatinib (hydrochloride) (Standard) is the analytical standard of Ponatinib (hydrochloride). This product is intended for research and analytical applications. Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib 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.
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Cediranib (Standard)
0 ImagesSynonyms: AZD2171 (Standard)Cediranib (Standard) is the analytical standard of Cediranib. This product is intended for research and analytical applications. Cediranib (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.
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Telatinib mesylate (Standard)
0 ImagesSynonyms: Bay 57-9352 mesylate (Standard)Telatinib (mesylate) (Standard) is the analytical standard of Telatinib (mesylate). This product is intended for research and analytical applications. Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.
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ENMD-2076 Tartrate (Standard)
0 ImagesCat. No.: HY-10987RCAS No.: 1453868-32-0ENMD-2076 Tartrate (Standard) is the analytical standard of ENMD-2076 (Tartrate) (HY-10987). This product is intended for research and analytical applications. ENMD-2076 Tartrate is a multi-targeted Kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KdR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
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Avapritinib (Standard)
0 ImagesSynonyms: BLU-285 (Standard)Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.
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PDGFRα Kinase inhibitor 1 (Standard)
0 ImagesCat. No.: HY-111507RCAS No.: 2209053-93-8PDGFRα Kinase inhibitor 1 (Standard) is the analytical standard of PDGFRα Kinase inhibitor 1 (HY-111507). This product is intended for research and analytical applications. 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.
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Pazopanib (Standard)
0 ImagesSynonyms: GW786034 (Standard)Pazopanib (Standard) is the analytical standard of Pazopanib. This product is intended for research and analytical applications. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
