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.
-
PDGFR Related Products (186)
Related Products (186)
-
KIT/PDGFRA-IN-3
0 ImagesCat. No.: HY-189238KIT/PDGFRA-IN-3 is a KIT and PDGFRA mutant kinase inhibitor, with an IC50 of 9 nM against human PDGFRA. KIT/PDGFRA-IN-3 inhibits the kinase activity of KIT, exhibiting superior selectivity for mutant KIT over wild-type KIT. KIT/PDGFRA-IN-3 suppresses the kinase activity of PDGFRA and blocks downstream signaling pathways. KIT/PDGFRA-IN-3 can be used in studies of gastrointestinal stromal tumors.
-
PDGFRα/FLT3-ITD-IN-2
0 ImagesCat. No.: HY-145903CAS No.: 2761259-09-8PDGFRα/FLT3-ITD-IN-2 (Compound 13d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 20 and 1.654 μM, respectively. PDGFRα/FLT3-ITD-IN-2 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia.
-
KN1022
0 ImagesCat. No.: HY-149462CAS No.: 205255-11-4KN1022 an inhibitor of phosphorylation of platelet-derived growth factor receptor (PDGFR) with IC50 of 0.24 μM.
-
Pazopanib Hydrochloride (Standard)
0 ImagesSynonyms: GW786034 Hydrochloride (Standard)Pazopanib (Hydrochloride) (Standard) is the analytical standard of Pazopanib (Hydrochloride). This product is intended for research and analytical applications. 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.
-
Regorafenib-13C,d3
0 ImagesCat. No.: HY-10331S1Synonyms: BAY 73-4506-13C,d3
-
Biotin-PDGFRβ Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70803PDGF-BB/PDGFRβ signaling plays an important role during vascularization by mediating pericyte recruitment to the vasculature, promoting the integrity and function of vessels. Biotin-PDGFRβ Recombinant Human Active Protein Kinase is a recombinant PDGFRβ protein that can be used to study PDGFRβ-related functions, and is biotinylated.
-
ON012380
0 ImagesCat. No.: HY-10365CAS No.: 592543-24-3ON012380 is a kinase inhibitor with an IC50 of 9 nM against BCR-ABL. As a substrate-competitive BCR-ABL inhibitor, ON012380 binds to a non-ATP site, and inhibits the kinase activities of PDGFR, Fyn and LynB at higher concentrations. ON012380 induces apoptosis, inhibits STAT-5 phosphorylation, reduces cell viability and suppresses cell growth in leukemia cells. ON012380 can be used in the research of chronic myeloid leukemia and Imatinib (HY-15463)-resistant chronic myeloid leukemia.
-
Tyrphostin A9 (Standard)
0 ImagesSynonyms: Tyrphostin 9 (Standard); Malonoben (Standard)Tyrphostin A9 (Standard) is the analytical standard of Tyrphostin A9. This product is intended for research and analytical applications. Tyrphostin A9, a PDGFR inhibitor, is a potent inducer of mitochondrial fission. Tyrphostin A9 emerged as the most potent and selective of 51 tyrosine kinase inhibitors tested against the TNF-induced respiratory burst. Tyrphostin A9 has anti-influenza virus activities.
-
Cediranib maleate (Standard)
0 ImagesSynonyms: AZD-2171 maleate (Standard)Cediranib (maleate) (Standard) is the analytical standard of Cediranib (maleate). This product is intended for research and analytical applications. Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
-
Masitinib mesylate (Standard)
0 ImagesSynonyms: AB-1010 mesylate (Standard)Masitinib (mesylate) (Standard) is the analytical standard of Masitinib (mesylate). This product is intended for research and analytical applications. Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity.
-
Toceranib phosphate (Standard)
0 ImagesCat. No.: HY-10330ARCAS No.: 874819-74-6Synonyms: SU11654 phosphate (Standard); PHA 291639E phosphate (Standard)Toceranib phosphate (Standard) is the analytical standard of Toceranib phosphate (HY-10330A). This product is intended for research and analytical applications. Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .
-
RPR-101511
0 ImagesCat. No.: HY-172228CAS No.: 146535-06-0RPR-101511 is a 3-substituted quinoline derivative. RPR-101511 is a PDGF receptor tyrosine kinase inhibitor (IC50: 0.001-0.02 μM).
-
Orantinib (Standard)
0 ImagesCat. No.: HY-10517RCAS No.: 252916-29-3Synonyms: SU6668 (Standard); TSU-68 (Standard)Orantinib (Standard) is the analytical standard of Orantinib (HY-10517). This product is intended for research and analytical applications. 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.
-
Dovitinib (Standard)
0 ImagesSynonyms: CHIR-258 (Standard); TKI258 (Standard)Dovitinib (Standard) is the analytical standard of Dovitinib. This product is intended for research and analytical applications. Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity.
-
Amuvatinib (Standard)
0 ImagesSynonyms: MP470 (Standard); HPK 56 (Standard)Amuvatinib (Standard) is the analytical standard of Amuvatinib. This product is intended for research and analytical applications. Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
-
(Z)-Orantinib (Standard)
0 ImagesCat. No.: HY-10517ARCAS No.: 210644-62-5Synonyms: (Z)-SU6668 (Standard); (Z)-TSU-68 (Standard)(Z)-Orantinib (Standard) is the analytical standard of (Z)-Orantinib (HY-10517A). This product is intended for research and analytical applications. (Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 μM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.
-
AGL 2043
0 ImagesCat. No.: HY-112350CAS No.: 226717-28-8AGL 2043 is an effective inhibitor of PDGFR (IC50=0.8 μM) and TEL-PDGFR kinases, as well as FLT3 and KIT kinases. AGL 2043 can effectively inhibit porcine cardiac smooth muscle cell proliferation and balloon-induced vascular stenosis, and is suitable for development as an anti-restenotic and anticancer agent.
-
Nintedanib esylate (Standard)
0 ImagesSynonyms: BIBF 1120 esylate (Standard)Nintedanib esylate (Standard) is the analytical standard of Nintedanib esylate. This product is intended for research and analytical applications. Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
-
Regorafenib (Standard)
0 ImagesSynonyms: BAY 73-4506 (Standard)Regorafenib (Standard) is the analytical standard of Regorafenib. This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.
