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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Tandutinib hydrochloride (Standard)
0 ImagesSynonyms: MLN518 hydrochloride (Standard); CT53518 hydrochloride (Standard)Tandutinib (hydrochloride) (Standard) is the analytical standard of Tandutinib (hydrochloride). This product is intended for research and analytical applications. Tandutinib hydrochloride (MLN518 hydrochloride) 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 hydrochloride can be used for acute myelogenous leukemia (AML). Tandutinib hydrochloride has the ability to cross the blood-brain barrier.
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Avapritinib-d3
0 ImagesCat. No.: HY-W754911CAS No.: 2408934-57-4Synonyms: BLU-285-d3Avapritinib-d3 (BLU-285-d3) is deuterium labeled Avapritinib. 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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Pazopanib-d3
0 ImagesCat. No.: HY-10208S2CAS No.: 1219591-97-5Synonyms: GW786034-d3
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XL 999 (Standard)
0 ImagesCat. No.: HY-100315RCAS No.: 705946-27-6Synonyms: Tyrosine kinase-IN-1 (Standard)XL 999 (Standard) is the analytical standard of XL 999 (HY-100315). This product is intended for research and analytical applications. XL999 is a multi-target tyrosine kinase inhibitor. XL999 has IC50 values for KDR, Flt-1, FGFR1 and PDGFRα of 4 nM, 20 nM, 4 nM and 2 nM, respectively. XL999 can be used in the research of cancer.
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cis-SU4312
0 ImagesCat. No.: HY-100349ACAS No.: 90828-16-3Synonyms: (Z)-SU4312
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Tyrphostin AG1296 (Standard)
0 ImagesCat. No.: HY-13894RCAS No.: 146535-11-7Synonyms: AG1296 (Standard)Tyrphostin AG1296 (Standard) is the analytical standard of Tyrphostin AG1296. This product is intended for research and analytical applications. Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
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Famitinib (Standard)
0 ImagesCat. No.: HY-108713RCAS No.: 1044040-56-3Synonyms: SHR1020 (Standard)Famitinib (Standard) is the analytical standard of Famitinib. This product is intended for research and analytical applications. Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis.
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Imatinib-13C,d3
0 ImagesCat. No.: HY-15463S3Synonyms: STI571-13C,d3; CGP-57148B-13C,d3Imatinib-13C,d3 (STI571-13C,d3) is 13C labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
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Sch 13835
0 ImagesCat. No.: HY-123392CAS No.: 150519-34-9Sch 13835 is a platelet-derived growth factor (PDGFR) inhibitor.
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PP121 (Standard)
0 ImagesCat. No.: HY-10372RCAS No.: 1092788-83-4
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2,6-Dihydroxyacetophenone-4-O-[4,6-(S)-hexahydroxydiphenoyl]-β-D-glucose
![2,6-Dihydroxyacetophenone-4-O-[4,6-(S)-hexahydroxydiphenoyl]-β-D-glucose](https://file.medchemexpress.com/product_pic/hy-n8032.gif "Click to View 2,6-Dihydroxyacetophenone-4-O-[4,6-(S)-hexahydroxydiphenoyl]-β-D-glucose Product Detail")
0 ImagesCat. No.: HY-N8032CAS No.: 1781226-44-52,6-Dihydroxyacetophenone-4-O-[4,6-(S)-hexahydroxydiphenoyl]-β-D-glucose is a novel polyphenol/ellagitannin-type glucoside. 2,6-Dihydroxyacetophenone-4-O-[4,6-(S)-hexahydroxydiphenoyl]-β-D-glucose mediates antiproliferative effects via platelet-derived growth factor (PDGF)-induced hepatic stellate cells. 2,6-Dihydroxyacetophenone-4-O-[4,6-(S)-hexahydroxydiphenoyl]-β-D-glucose can be used for the research of hepatic fibrosis.
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Linifanib (Standard)
0 ImagesCat. No.: HY-50751RCAS No.: 796967-16-3Synonyms: ABT-869 (Standard); AL-39324 (Standard)Linifanib (Standard) is the analytical standard of Linifanib. This product is intended for research and analytical applications. Linifanib (ABT-869) 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 shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
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Sunitinib-d4
0 ImagesCat. No.: HY-10255AS1CAS No.: 1126721-79-6Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
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TG 100572 hydrochloride (Standard)
0 ImagesCat. No.: HY-10185RCAS No.: 867331-64-4TG 100572 hydrochloride (Standard) is the analytical standard of TG 100572 hydrochloride (HY-10185). This product is intended for research and analytical applications. TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
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Telatinib (Standard)
0 ImagesCat. No.: HY-10527RCAS No.: 332012-40-5Synonyms: Bay 57-9352 (Standard)Telatinib (Standard) is the analytical standard of Telatinib. This product is intended for research and analytical applications. Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
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Tandutinib (Standard)
0 ImagesCat. No.: HY-10202RCAS No.: 387867-13-2Synonyms: MLN518 (Standard); CT53518 (Standard)Tandutinib (Standard) is the analytical standard of Tandutinib. This product is intended for research and analytical applications. Tandutinib (MLN518) 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 can be used for acute myelogenous leukemia (AML). Tandutinib has the ability to cross the blood-brain barrier.
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Anti-Mouse PDGFRα Antibody (APA5)
0 ImagesCat. No.: HY-P991758Anti-Mouse PDGFRα Antibody (APA5) reacts with mouse PDGFRα. Anti-Mouse PDGFRα Antibody (APA5) can be used to block PDGFRα in vitro and in vivo. Anti-Mouse PDGFRα Antibody (APA5) can be used for the study of pulmonary hypertension. Recommend Isotype Controls: Rat IgG2a kappa, Isotype Control (HY-P990679).
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Seralutinib (Standard)
0 ImagesCat. No.: HY-109190RCAS No.: 1619931-27-9Synonyms: GB002 (Standard); PK10571 (Standard)Seralutinib (Standard) is the analytical standard of Seralutinib (HY-109190). This product is intended for research and analytical applications. Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib also targets to CSF1R and c-KiT with IC50s of 8 nM and 14 nM, respectively. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.
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Toceranib (Standard)
0 ImagesCat. No.: HY-10330RCAS No.: 356068-94-5Synonyms: SU11654 (Standard); PHA 291639E (Standard)Toceranib (Standard) is the analytical standard of Toceranib (HY-10330). 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.
