Drug Class Detail

Drug Class CSF1R Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Sorafenib Nexavar BAY 43-9006 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RAF Inhibitor (Pan) 17 RET Inhibitor 36 VEGFR2 Inhibitor 34 Nexavar (sorafenib) is a multikinase inhibitor with activity against several kinases, including RAF kinases, VEGFR2, VEGFR3, PDGFR-beta, KIT, FLT3, RET, and CSF1R, potentially resulting in decreased tumor growth (PMID: 18445656, PMID: 15466206, PMID: 21517818). Nexavar (sorafenib) is approved for metastatic differentiated thyroid carcinoma, hepatocellular carcinoma, and renal cell carcinoma (FDA.gov).
JNJ-40346527 CSF1R Inhibitor 22 JNJ-40346527 is a small molecule inhibitor of CSF1R, which may inhibit growth of CSF1R-expressing tumor cells (PMID: 25628399).
Imatinib mesylate Gleevec CGP-57148B|STI571 ABL Inhibitor (pan) 8 BCR-ABL Inhibitor 23 CSF1R Inhibitor 22 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 Gleevec (imatinib mesylate) is a multi-target inhibitor of c-Kit, Pdgfr, and Bcr-Abl (NCI Drug Dictionary). Gleevec (imatinib mesylate) is FDA approved for c-KIT positive GIST and dermatofibrosarcoma protuberans, Philadelphia chromosome positive chronic myeloid leukemia, and FIP1L1-PDGFRA positive chronic eosinophilic leukemia (FDA.gov).
DCC-3014 CSF1R Inhibitor 22 DCC-3014 inhibits CSF1R, potentially resulting in increased anti-tumor immune response in combination with other agents (Cancer Res 2016;76(14 Suppl):Abstract nr 4889).
Chiauranib CS2164 Aurkb Inhibitors 17 CSF1R Inhibitor 22 KIT Inhibitor 48 PDGFR-alpha Inhibitor 7 VEGFR Inhibitor (Pan) 29 Chiauranib (CS2164) is a multi-kinase inhibitor that inhibits AURKB, CSF-1R, VEGFRs, KIT, and PDGFRA, resulting in decreased tumor growth and angiogenesis (PMID: 28004478).
AC708 PLX73086 CSF1R Inhibitor 22 PLX73086 (AC708) is a small molecule inhibitor of CSF1R, which leads to reduced CSF1R activation and may restore resistance to angiogenesis inhibition through a decrease in tumor associated macrophages (PMID: 29228548).
Sunitinib Sutent SU011248 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 RET Inhibitor 36 VEGFR2 Inhibitor 34 Sutent (sunitinib) inhibits KDR (VEGFR2), PDGFR, c-KIT, FLT3, RET, and CSF1R, thereby inhibiting angiogenesis and cell proliferation (NCI Drug Dictionary; PMID: 25085632). Sutent (sunitinib) is approved for neuroendocrine tumors of the pancreas, advanced renal cell carcinoma, and GIST (FDA.gov).
Linifanib ABT-869|AL-39324 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 VEGFR Inhibitor (Pan) 29 Linifanib (ABT-869) is a receptor tyrosine kinase inhibitor with specificity against FLT1 (VEGFR1), CSF-1R, KDR (VEGFR2), FLT3, and KIT, which may result in inhibition of cell proliferation and tumor growth, and tumor regression (PMID: 16648571).
Dasatinib Sprycel BMS-354825 ABL Inhibitor (pan) 8 BCR-ABL Inhibitor 23 BTK inhibitor 20 CSF1R Inhibitor 22 DDR1 Inhibitor 8 DDR2 inhibitor 7 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 SRC Inhibitor 26 TNK2 Inhibitor 6 Sprycel (dasatinib) is an inhibitor of the SRC-family of protein kinases, BCR-ABL, and ABL, and has additional activity against other kinases including KIT, DDR1/2, PDGFRA/B, and EPHA2, which prevents cell growth (PMID: 25709401, PMID: 25284748, PMID: 18797457). Sprycel (dasatinib) is FDA approved for both Philadelphia chromosome positive adult and pediatric chronic myelogenous leukemia and adult acute lymphoblastic leukemia (FDA.gov).
BLZ945 CSF1R Inhibitor 22 BLZ945 is a selective inhibitor of CSF1R, which potentially leads to a decrease in tumor associated macrophages (PMID: 24498562).
Midostaurin Rydapt PKC412|CGP 41251 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 PKC alpha Inhibitor 6 PKC beta Inhibitor 6 PKC Inhibitor (Pan) 9 VEGFR2 Inhibitor 34 Rydapt (midostaurin) is a multi-kinase inhibitor with activity against FLT3, KIT, PDGFRB, KDR (VEGFR2) and PKC, with higher selectivity for conventional PKC isoforms, which induces cell cycle arrest and apoptosis (PMID: 12124173, PMID: 23127174, PMID: 15914319). Rydapt (midostaurin) is FDA approved for FLT3-mutant AML in combination with chemotherapy, and is approved for use in aggressive systemic mastocytosis, systemic mastocytosis with associated hematological neoplasm, or mast cell leukemia as a single therapy (FDA.gov).
Ki20227 CSF1R Inhibitor 22 Ki20227 inhibits CSF1R, which may result in decreased CSF-dependent cell growth (PMID: 17121910).
Debio 0617B ABL Inhibitor (pan) 8 CSF1R Inhibitor 22 FLT3 Inhibitor 48 JAK Inhibitor (Pan) 8 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 29 Debio 0617B is a multi-kinase inhibitor of SRC, JAK, and ABL, the class III kinases, CSF1R, FLT3, KIT, and PDGFR, and the class V kinases, VEGFR 1/2/3, which may result in inhibition of Stat3 and Stat5 signaling, leading to inhibition of tumor cell growth and metastasis (PMID: 27439479).
Lestaurtinib CEP-701 CSF1R Inhibitor 22 FLT3 Inhibitor 48 JAK2 Inhibitor - ATP competitive 14 Trk Receptor Inhibitor (Pan) 21 Lestaurtinib (CEP-701) inhibits JAK2, FLT3 and NTRK1-3, resulting in antiproliferative activity (PMID: 17143529, PMID: 17442779, PMID: 17984313).
Emactuzumab RG7155|RO5509554 CSF1R Inhibitor 22 Emactuzumab (RG7155) is a monoclonal antibody that inhibits dimerization of CSF1R, resulting in decreased ligand-dependent and ligand-independent signaling, thereby potentially leading to reduced tumor growth (PMID: 24898549).
FF-10101 FF-10101-01 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 FF-10101 is a second generation and irreversible inhibitor of Flt3, including the internal tandem duplication (FLT3-ITD) and known resistance mutations (D835Y, Y842C, Y842H, or F691L) and also inhibits Kit and Csf1r (Fms) (PMID: 29187377)
Dovitinib TKI258|CHIR-258 CSF1R Inhibitor 22 FGFR Inhibitor (Pan) 17 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 VEGFR Inhibitor (Pan) 29 Dovitinib (TKI258) targets multiple receptor tyrosine kinases including Flt3, c-Kit, CSF1R, FGFR 1-4, VEGFR 1-3, and PDGFR alpha and beta, potentially resulting in decreased tumor growth (PMID: 15598814, PMID: 25219510, PMID: 23658459, PMID: 16033847).
PLX7486 CSF1R Inhibitor 22 Trk Receptor Inhibitor (Pan) 21 PLX7486 binds to and inhibits CSF1R, TRKA, TRKB, and TRKC, which potentially results in decreased tumor cell proliferation (NCI Drug Dictionary).
GW2580 CSF1R Inhibitor 22 GW2580 is an ATP-competitive selective inhibitor of CSF-1R, which may lead to decreased tumor cell growth (PMID: 16249345, PMID: 23372702).
Pexidartinib PLX3397 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 Pexidartinib (PLX3397) inhibits multiple receptor tyrosine kinases, including KIT, CSF1R, FLT3, and FLT3/ITD, which may inhibit growth in cancer cells (PMID: 22294205, PMID: 25993548, PMID: 25847190).
Nilotinib Tasigna AMN-107 ABL Inhibitor (pan) 8 BCR-ABL Inhibitor 23 CSF1R Inhibitor 22 DDR1 Inhibitor 8 DDR2 inhibitor 7 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 Tasigna (nilotinib) inhibits several tyrosine kinases including BCR-ABL, PDGFR, KIT, DDR and CSF-1R, potentially resulting in reduced tumor cell proliferation (PMID: 21419934, PMID: 25284748). Tasigna (nilotinib) is FDA approved for use in patients with Ph+ chronic myeloid leukemia (FDA.gov).
ARRY-382 CSF1R Inhibitor 22 ARRY-382 is a small molecule inhibitor of CSF1R, which potentially leads to decreased growth of CSF1R over expressing tumor cells (NCI Drug Dictionary).
Molecular Profile Protein Effect Treatment Approaches
CSF1R Y969F unknown CSF1R Inhibitor
CSF1R D802V gain of function CSF1R Inhibitor
CSF1R act mut gain of function CSF1R Inhibitor
CSF1R L301S gain of function CSF1R Inhibitor
CSF1R Y571D gain of function CSF1R Inhibitor