Catalog No.
Product Name
Application
Product Information
Citations
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multi-targeted receptor tyrosine kinase inhibitor
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Wei Kang Cheng, .et al. , Microvasc Res, 2022, Feb 11;142:104341 PMID: 35157839
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KIT and PDGFRA inhibitor
Avapritinib (BLU-285) is a highly potent, selective, and orally bioavailable KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. -
KIT and PDGFRA switch-control inhibitor
Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. -
type II PDGFRα kinase inhibitor
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. -
ATP-competitive multitargeted kinase inhibitor
Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. -
Raf/VEGFR3 inhibitor
Sorafenib D3 (Bay 43-9006 D3) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively. -
Raf/VEGFR3 inhibitor
Sorafenib D4 (Bay 43-9006 D4) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively. -
multi-targeted tyrosine kinase inhibitor
Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. -
multi-targeted kinase inhibitor
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. -
PDGFR inhibitor
Seralutinibm, also known as PK-10571 and GB002, is a Inhaled Pdgfr Kinase Inhibitor. -
PDGFRα/PDGFRβ inhbitor
JNJ 10198409 is a potent platelet-derived growth factor receptor (PDGFR) inhibitor (IC50 values are 4.2 and 45 nM for PDGFRβ and PDGFRα, respectively). Also inhibits c-Abl, Lck, c-Src and Fyn kinases (IC50 values are 22, 100, 185 and 378 nM respectively). -
multi-kinase inhibitor
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. -
SU-4313 is a small-molecule modulator of protein tyrosine kinases (PTKs). It inhibits multiple receptor tyrosine kinases with reported IC₅₀ values of 14.5 μM (PDGFR), 18.8 μM (FLK-1/VEGFR2), 11 μM (EGFR), 16.9 μM (HER2 kinase), and 8.0 μM (IGF-1R).
Through its multi-kinase inhibitory profile, SU-4313 modulates tyrosine kinase–mediated signal transduction pathways involved in the regulation of cell proliferation and growth. It is therefore commonly used as a research tool for investigating aberrant receptor tyrosine kinase signaling and proliferation-associated pathways.
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PDGFR Inhibitor
Methylnissolin (Astrapterocarpan), a natural compound isolated from *Astragalus membranaceus*, inhibits PDGF-BB-induced vascular smooth muscle cell proliferation with an IC50 of 10 μM. It exerts its effects by suppressing PDGF-BB-induced phosphorylation of ERK1/2, thereby blocking activation of the ERK1/2 MAP kinase signaling cascade. -
PDGFRβ/VEGFR-2 inhibitor
Tyrphostin AG1433 (SU1433) is a tyrosine kinase inhibitor that selectively targets platelet-derived growth factor receptor beta (PDGFRβ) and vascular endothelial growth factor receptor 2 (VEGFR-2/Flk-1/KDR), with IC₅₀ values of 5.0 μM and 9.3 μM, respectively. By inhibiting these key angiogenic receptors, AG1433 disrupts downstream signaling involved in endothelial cell proliferation and migration, thereby effectively preventing blood vessel formation (angiogenesis). It is a valuable compound for research into tumor angiogenesis, vascular disorders, and anti-angiogenic therapeutic strategies. -
Multi-target Inhibitor
Chiauranib (CS2164) is an orally active, multi-targeted small molecule inhibitor with potent anticancer activity. It targets key kinases involved in tumor angiogenesis, including VEGFR1, VEGFR2, VEGFR3, PDGFRα, and c-Kit, as well as mitosis-related kinase Aurora B and inflammation-associated kinase CSF-1R. Chiauranib exhibits IC₅₀ values ranging from 1 to 9 nM against these targets. Through simultaneous inhibition of angiogenesis, cell division, and inflammation pathways, Chiauranib exerts strong antitumor effects and is a promising candidate for the treatment of various solid tumors. -
PDGFR Inhibitor
Sennoside B is a potent inhibitor of platelet-derived growth factor receptor (PDGFR). It effectively suppresses cell proliferation and reduces the phosphorylation of PDGFR-β, STAT-5, AKT, and ERK in response to PDGF-BB stimulation. Additionally, Sennoside B exhibits gastroprotective properties and is suitable for research applications focused on gastritis and related gastrointestinal disorders. -
PDGFRα/β/Bcr-Abl Inhibitor
GZD856 formic is a selective inhibitor of PDGFRα/β, displaying IC50 values of 68.6 nM and 136.6 nM, respectively, along with potent inhibition of Bcr-Abl, including the T315I mutant with IC50s of 19.9 nM and 15.4 nM. This compound exhibits notable antitumor activity, making it a valuable tool for cancer research. Additionally, GZD856 formic serves as a click chemistry reagent due to its alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating bioconjugation studies and compound labeling. -
PDGFR Inhibitor
PDGFR-IN-1 is a potent inhibitor of the platelet-derived growth factor receptor (PDGFR), exhibiting IC50 values of 2.4 nM for PDGFRα and 0.9 nM for PDGFRβ. This compound demonstrates significant antitumor activity while maintaining low toxicity, making it a valuable tool for research applications in osteosarcoma studies. Its selectivity for PDGFR allows for detailed investigations into tumor growth mechanisms and therapeutic interventions. -
c-kit/VEGFR/PDGFR Inhibitor
Famitinib malate is an orally active, multi-targeted kinase inhibitor primarily targeting c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This compound induces cell apoptosis and demonstrates significant anti-tumor activity in human gastric cancer cells and xenograft models. Famitinib malate is a valuable tool for research into cancer therapies and mechanisms of action. -
c-kit/VEGFR/PDGFR Inhibitor
Famitinib is a potent multi-targeted kinase inhibitor that primarily targets c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This orally active compound demonstrates significant antitumor activity in human gastric cancer cells and xenograft models. Famitinib also induces apoptosis, making it a valuable tool for research in cancer therapeutics and signaling pathways. -
PDGFR Inhibitor
(Z)-Orantinib is a selective, orally active ATP-competitive inhibitor targeting PDGFRβ, as well as Flk‐1/KDR and FGFR1, with IC50 values of 0.008 µM, 2.1 µM, and 1.2 µM, respectively. This compound exhibits significant antiangiogenic and antitumor properties, effectively inducing regression of established tumors. It is a valuable tool for research applications focused on cancer biology and the mechanisms of angiogenesis. -
PDGFRβ/B-Raf Inhibitor
KG5 is an orally active dual inhibitor targeting PDGFRβ and B-Raf through allosteric mechanisms. It also exhibits inhibitory effects on Flt3, KIT, and c-Raf. KG5 demonstrates significant anticancer and antiangiogenic activities, making it a valuable reagent for research in cancer therapy and angiogenesis studies. -
PDGFRα/FLT3 Inhibitor
PDGFRα/FLT3-ITD-IN-3 is a highly effective inhibitor of PDGFRα and FLT3, exhibiting IC50 values of 0.153 μM and 0.004 μM, respectively. This compound serves as a valuable tool in the investigation of acute myeloid leukemia and chronic eosinophilic leukemia. Its potent inhibitory activity against key receptors makes it a significant candidate for related biomedical research applications. -
PDGFRα/FLT3 Inhibitor
PDGFRα/FLT3-ITD-IN-1 is a selective inhibitor of the platelet-derived growth factor receptor alpha (PDGFRα) and the Fms-like tyrosine kinase 3 (FLT3), demonstrating IC50 values of 0.036 μM and 0.003 μM, respectively. This compound is particularly relevant for investigations into acute myeloid leukemia (AML) and chronic eosinophilic leukemia (CEL), providing a valuable tool for exploring therapeutic strategies targeting these malignancies. Researchers utilizing PDGFRα/FLT3-ITD-IN-1 can gain insights into the molecular mechanisms underlying these hematological disorders. -
PDGFRα/FLT3 Inhibitor
PDGFRα/FLT3-ITD-IN-2 is a selective inhibitor targeting PDGFRα and FLT3, exhibiting IC50 values greater than 20 μM and 1.654 μM, respectively. This compound demonstrates significant biological activity relevant to the treatment of acute myeloid leukemia and chronic eosinophilic leukemia. Its efficacy in modulating these pathways makes it a valuable tool for investigational research in cancer therapeutics. -
PDGFR/TEL-PDGFR/FLT3/KIT Inhibitor
AGL 2043 is a potent inhibitor of PDGFR, TEL-PDGFR, FLT3, and KIT kinases, exhibiting an IC50 value of 0.8 μM against PDGFR. This compound demonstrates significant biological activity by effectively reducing porcine cardiac smooth muscle cell proliferation and mitigating balloon-induced vascular stenosis. AGL 2043 presents promising applications in the development of anti-restenotic and anticancer therapies. -
VEGFR/PDGFR Inhibitor
BMS-605541 is a selective, orally active inhibitor targeting VEGFR-2 kinase, exhibiting an IC50 of 23 nM and a Ki of 49 nM. It also inhibits Flk-1, VEGFR-1, and PDGFR-β with IC50 values of 40 nM, 400 nM, and 200 nM, respectively. This reagent is valuable for cancer research, aiding in the study of angiogenesis and tumor progression. -
PDGFR Inhibitor
cis-SU4312 is a potent inhibitor of the Platelet-Derived Growth Factor Receptor (PDGFR) and FLK-1, exhibiting IC50 values of 19.4 μM and 0.8 μM, respectively. Additionally, cis-SU4312 targets several other receptors, including EGFR, HER-2, and IGF-1R with IC50 values of 24.2 μM, 18.5 μM, and 10.0 μM, respectively. Due to its ability to cross the blood-brain barrier, cis-SU4312 is valuable in research applications related to cancer biology and neurobiology. -
PDGFRβ Inhibitor
SU16f is a potent and selective inhibitor of PDGFRβ, exhibiting IC50 values of 10 nM for PDGFRβ, 140 nM for VEGF-R2, and 2.29 μM for FGF-R1. By effectively neutralizing the PDGFRβ receptor, SU16f disrupts the supportive effects of gastric cancer-derived mesenchymal stem cells (GC-MSCs) conditioned medium on gastric cancer cell proliferation and migration. This compound is valuable for research applications focused on gastric cancer and the modulation of tumor microenvironments. -
PDGFR Inhibitor
PDGFR Tyrosine Kinase Inhibitor III is a potent inhibitor of platelet-derived growth factor receptor (PDGFR), along with other kinases such as EGFR, FGFR, PKA, and PKC. This multikinase inhibitor plays a crucial role in modulating various signaling pathways involved in cellular proliferation and survival. Its application extends to the investigation of amyotrophic lateral sclerosis, providing insights into the underlying mechanisms of this neurodegenerative disorder. Researchers can employ this compound to explore therapeutic strategies targeting PDGFR and associated pathways. -
PDGFR Inhibitor
WQ-C-401 is an orally active inhibitor of the platelet-derived growth factor receptor (PDGFR), effectively blocking PDGFR autophosphorylation with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. This compound significantly inhibits the proliferation and migration of pulmonary artery smooth muscle cells (PASMCs) by interfering with PDGF-BB-induced ERK1/2 phosphorylation, thus reducing collagen I synthesis and enhancing α-smooth muscle actin expression. WQ-C-401 is a valuable tool for studying mechanisms underlying pulmonary vascular remodeling and holds potential for research in pulmonary arterial hypertension. -
PDGFR Antagonist
CT52923 is a selective antagonist of the platelet-derived growth factor receptor (PDGFR) and acts as an ATP-competitive inhibitor. This compound demonstrates significant biological activity relevant to a range of pathological conditions, including atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and certain cancers. CT52923 can be utilized to explore therapeutic pathways and mechanisms involved in these diseases. -
PDGFr Inhibitor
PDGFR-IN-2 is a 4-phenoxyquinoline derivative that acts as a selective inhibitor of the platelet-derived growth factor receptor (PDGFr) with an IC50 value of 0.20 μM. By targeting PDGFr tyrosine kinase activity, PDGFR-IN-2 effectively disrupts downstream signaling pathways associated with cell proliferation and migration. This compound is valuable for research applications investigating the role of PDGFr in various pathological conditions, including cancer and fibrotic diseases. -
PDGFR Inhibitor
DMPQ dihydrochloride is a selective inhibitor of human platelet-derived growth factor receptor β (PDGFRβ), exhibiting an IC50 of 80 nM. This compound demonstrates significant potential in research applications focused on PDGFRβ-mediated signaling pathways, which are implicated in a variety of pathological conditions, including cancer and fibrosis. Its potency and selectivity make DMPQ dihydrochloride a valuable tool for investigating the role of PDGFRβ in cellular processes and therapeutic interventions. -
PDGFR Inhibitor
AG 370 is a selective inhibitor of the platelet-derived growth factor receptor (PDGFR), exhibiting potent activity against PDGF-induced mitogenesis with an IC50 of 20 μM. Additionally, AG 370 demonstrates weak inhibitory effects on the epidermal growth factor receptor (EGFR). This compound is valuable for research applications focused on signaling pathways related to cell proliferation and cancer biology. -
PDGFR-α Inhibitor
PDGFRα kinase-IN-2 is a potent inhibitor of the platelet-derived growth factor receptor alpha (PDGFR-α) with an IC50 of 2.1 nM. This compound exhibits significant anticancer activity against HT-29 human colon cancer cells, with an IC50 of 1.48 μM. Additionally, PDGFRα kinase-IN-2 demonstrates anti-angiogenic properties in zebrafish models while exhibiting low embryonic lethality. It is a valuable tool for research focused on colon cancer and the mechanisms of anti-angiogenesis. -
TGFβRI/PDGFRα Inhibitor
BI-4659 is a dual inhibitor of TGFβRI and PDGFRα, exhibiting IC50 values of 19 nM and 99 nM, respectively. This compound effectively inhibits the kinase activities of both receptors, thereby blocking downstream TGFβRI signaling and reducing Smad2/3 phosphorylation without impacting TGF-β1 expression. BI-4659 is suitable for research applications in pulmonary fibrosis, cancer, and renal ischemia-reperfusion injury studies. -
PDGFR Fragment
PDGFR Y1021 peptide (non-phosphorylation) is a specific non-phosphorylated fragment of the platelet-derived growth factor receptor (PDGFR). This peptide effectively inhibits the association of PLCγ with PDGFR via the PLCγ SH2 domain, thereby blocking the mitogenic response. It serves as a valuable tool in research focused on signaling pathways involving PDGFR and its role in cell growth and proliferation. -
PDGFRA Inhibitor
GSK190937 is a type II inhibitor of the platelet-derived growth factor receptor alpha (PDGFRA), exhibiting notable antimalarial activity. This compound effectively inhibits hemozoin formation in malaria parasites, leading to the accumulation of free hemoglobin. GSK190937 demonstrates IC50 values of 0.22 μM, 0.59 μM, and 0.25 μM against Plasmodium falciparum strains NF54, K1, and Dd2, respectively. Additionally, it has an IC50 of 25 μM for CHO cells, making it a valuable tool for malaria research. -
PDGFR Fragment
PDGFR Y1021 peptide (phosphorylation) is a phosphorylated fragment of the platelet-derived growth factor receptor (PDGFR) that facilitates the binding of phospholipase C-gamma (PLCγ) through its SH2 domains. This interaction enhances the production of inositol phosphates and stimulates mitogenic responses. The peptide serves as a valuable tool for research investigating PDGFR signaling pathways and their roles in cellular proliferation and differentiation. -
PDGFR Inhibitor
KN1022 is a selective inhibitor of the phosphorylation of platelet-derived growth factor receptor (PDGFR), with an IC50 value of 0.24 μM. This compound effectively modulates PDGFR signaling pathways, making it a valuable tool for investigating the role of PDGFR in various cellular processes. It is particularly relevant for research in cancer biology, fibrosis, and other diseases associated with abnormal PDGFR activity. -
PDGFR Inhibitor
Sch 13835 is a selective inhibitor of the platelet-derived growth factor receptor (PDGFR), which plays a critical role in cellular processes such as proliferation, differentiation, and survival. This compound exhibits significant inhibitory activity against PDGFR, making it a valuable tool for studying pathways involved in cancer and fibrosis. Its applications include investigating the role of PDGFR in tumor growth and exploring therapeutic strategies for conditions driven by aberrant PDGFR signaling.
