CSF-1R
Inhibitory Selectivity
CSF-1R Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1181 |
ENMD-2076ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2. |
Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
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| S8042 |
GW2580GW2580 (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. |
CSF1R c.1085A>G genetic variant confers the sensitivity of macrophage survival to CSF-1R inhibitors. Macrophages differentiated from peripheral blood mononuclear cells were incubated with various concentrations of the CSF-1R inhibitor, GW2580 (C) for 8 days. Percentage of cell survival was determined by CellTiter-Glo® Luminescent Cell Viability Assay. |
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| S7688 |
Ki20227Ki20227 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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| S3570 |
ARRY-382ARRY-382 is a highly selective, oral inhibitor of the CSF1R with an IC50 of 9 nM. |
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| S8578 |
PRN1371PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively. |
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| S7725 |
BLZ945BLZ945 is an orally active, potent and selective CSF-1R inhibitor with IC50 of 1 nM, >1000-fold selective against its closest receptor tyrosine kinase homologs. |
CSF1R c.1085A>G genetic variant confers the sensitivity of macrophage survival to CSF-1R inhibitors. Macrophages differentiated from peripheral blood mononuclear cells were incubated with various concentrations of the CSF-1R inhibitor, BLZ945 (B) for 8 days Percentage of cell survival was determined by CellTiter-Glo® Luminescent Cell Viability Assay. |
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| S8874 |
PLX5622PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3. |
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| S0487 |
SulfatinibSulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib) 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. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1181 |
ENMD-2076ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2. |
Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
|
|
| S8042 |
GW2580GW2580 (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. |
CSF1R c.1085A>G genetic variant confers the sensitivity of macrophage survival to CSF-1R inhibitors. Macrophages differentiated from peripheral blood mononuclear cells were incubated with various concentrations of the CSF-1R inhibitor, GW2580 (C) for 8 days. Percentage of cell survival was determined by CellTiter-Glo® Luminescent Cell Viability Assay. |
|
| S7688 |
Ki20227Ki20227 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. |
||
| S3570 |
ARRY-382ARRY-382 is a highly selective, oral inhibitor of the CSF1R with an IC50 of 9 nM. |
||
| S8578 |
PRN1371PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively. |
||
| S7725 |
BLZ945BLZ945 is an orally active, potent and selective CSF-1R inhibitor with IC50 of 1 nM, >1000-fold selective against its closest receptor tyrosine kinase homologs. |
CSF1R c.1085A>G genetic variant confers the sensitivity of macrophage survival to CSF-1R inhibitors. Macrophages differentiated from peripheral blood mononuclear cells were incubated with various concentrations of the CSF-1R inhibitor, BLZ945 (B) for 8 days Percentage of cell survival was determined by CellTiter-Glo® Luminescent Cell Viability Assay. |
|
| S8874 |
PLX5622PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3. |
||
| S0487 |
SulfatinibSulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib) 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. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs. |
