CSF-1R inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S7818 | Pexidartinib (PLX3397) | Pexidartinib (PLX3397) is an oral, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. This compound induces apoptosis and necrosis with antitumor activity. Phase 3. |
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| S7725 | Sotuletinib (BLZ945) | Sotuletinib (BLZ945) is an orally active, potent and selective CSF-1R inhibitor with an IC50 of 1 nM, and it is >1000-fold selective against its closest receptor tyrosine kinase homologs. |
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| S8042 | GW2580 | GW2580 (SC-203877) is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc. |
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| S8401 | Erdafitinib (JNJ-42756493) | Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. This compound also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis. |
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| S1189 | Aprepitant | Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. This compound reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. It inhibits HIV infection of human macrophages. |
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| S8874 | PLX5622 | PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3. |
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| S8524 | Edicotinib(JNJ-40346527) | Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. |
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| S7688 | Ki20227 | Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively. |
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| E0340 | CSF1R-IN-1 | CSF1R-IN-1 is a CSF1R (Colony Stimulating Factor 1 Receptor) inhibitor with an IC50 of 0.5 nM in vitro kinase activity assay. |
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| S0487 | Sulfatinib | Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. This compound shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs. |
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