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. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3. |
-
Nat Commun, 2024, 15(1):383
-
Brain Behav Immun, 2024, 119:621-636
-
J Neuroinflammation, 2024, 21(1):249
|
|
S3012 |
Pazopanib
|
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy. |
-
Cell Rep Med, 2024, S2666-3791(24)00201-5
-
Biomed Pharmacother, 2024, 180:117468
-
Transl Psychiatry, 2024, 14(1):166
|
|
S1035 |
Pazopanib HCl
|
Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death. |
-
iScience, 2023, 26(7):107116
-
NPJ Breast Cancer, 2022, 8(1):44
-
J Pers Med, 2022, 12(2)258
|
|
S1189 |
Aprepitant
|
Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. Aprepitant inhibits HIV infection of human macrophages. |
-
Br J Cancer, 2024, 10.1038/s41416-024-02608-8
-
Inflammation, 2023, 46(1):256-269
-
Nat Commun, 2022, 13(1):4995
|
|
S8401 |
Erdafitinib
|
Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis. |
-
J Clin Invest, 2024, 134(2)e169241
-
Adv Sci (Weinh), 2024, 11(16):e2303379
-
Clin Cancer Res, 2024, 10.1158/1078-0432.CCR-24-1834
|
|
S1003 |
Linifanib (ABT-869)
|
Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3. |
-
Cell Death Discov, 2023, 9(1):57
-
Cell Death Discov, 2023, 9(1):57
-
Cancer Cell, 2022, S1535-6108(22)00312-9
|
|
S7725 |
Sotuletinib (BLZ945)
|
Sotuletinib (BLZ945) 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.
|
-
Nat Commun, 2024, 15(1):1987
-
Immunity, 2023, 56(9):2152-2171.e13
-
J Exp Med, 2023, 220(3)e20220857
|
|
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. |
-
Sci Immunol, 2023, 10.1126/sciimmunol.adj5097
-
J Nanobiotechnology, 2023, 21(1):44
-
Brain Behav Immun, 2021, S0889-1591(21)00097-0
|
|
S1181 |
ENMD-2076
|
ENMD-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. |
-
Cell, 2021, 184(2):334-351.e20
-
Sci Adv, 2021, 7(4)eabd7851
-
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
|
|
S8874 |
PLX5622
|
PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3. |
-
Pharmacol Res, 2023, 196:106912
-
Cell Death Dis, 2023, 14(6):380
-
Cell Death Dis, 2023, 14(6):380
|
|
S1220 |
OSI-930
|
OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1. |
-
Nat Commun, 2024, 15(1):4739
-
Cell Rep, 2019, 28(9):2331-2344
-
Nat Biomed Eng, 2018, 2(8):578-588
|
|
S8015 |
Agerafenib (CEP-32496)
|
Agerafenib (CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2. |
-
Mol Pharmacol, 2021, 99(6):435-447
-
Dis Model Mech, 2020, dmm.047779
-
Cancer Immunol Res, 2019,
|
|
S8721 |
PDGFR inhibitor 1
|
PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth. |
-
Elife, 2023, 12e79840
-
Elife, 2023, 12e79840
-
Oncogene, 2022, 41(20):2860-2872
|
|
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. |
-
Biomed Pharmacother, 2024, 180:117554
-
J Exp Med, 2023, 220(3)e20220857
|
|
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. |
-
Life (Basel), 2022, 12(10)1676
|
|
S8578 |
PRN1371
|
PRN1371 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.
|
-
Int J Biol Sci, 2024, 20(9):3412-3425
-
Nat Commun, 2021, 12(1):6572
|
|
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. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs. |
-
Front Oncol, 2023, 13:1158857
|
|
E2629 |
Vimseltinib
|
Vimseltinib (DCC-3014) is a c-FMS (CSF-IR) and c-Kit dual inhibitor extracted from patent WO2014145025A2, Compound Example 10, has IC50s of <0.01 μM and 0.1-1 μM, respectively. |
|
|
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. |
-
Cancer Immunol Immunother, 2024, 73(5):76
-
Cancer Immunol Immunother, 2024, 73(5):76
|
|
S9620 |
Elzovantinib (TPX-0022)
|
Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models. |
|
|
S3523 |
AZD7507
|
AZD7507 is a potent and orally active CSF-1R inhibitor, with antitumor activity. |
|
|
A2644 |
Cabiralizumab (Anti-CSF1R / M-CSFR / CD115)
|
Cabiralizumab (Anti-CSF1R / M-CSFR / CD115) is an monoclonal antibody (MAb) targeting CSF1R. It can be used in the research of rheumatoid arthritis (RA), melanoma, kidney cancer, or non-small cell lung cancer. MW :146.3 KD. |
|
|
E0616 |
Chiauranib
|
Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy. |
|
|
S3570 |
ARRY-382
|
ARRY-382 is a highly selective, oral inhibitor of the CSF1R with an IC50 of 9 nM. |
|
|
E1435New |
Tinengotinib
|
Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC). |
|
|
E1727New |
Pimicotinib
|
Pimicotinib (ABSK021) is an orally bioavailable inhibitor of colony stimulating factor 1 receptor (CSF1R). It enhances antitumor T-cell immune responses and inhibits the proliferation of tumor cells having potential immunomodulatory and antineoplastic activities. |
|
|
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. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3. |
- Nat Commun, 2024, 15(1):383
- Brain Behav Immun, 2024, 119:621-636
- J Neuroinflammation, 2024, 21(1):249
|
|
S3012 |
Pazopanib
|
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy. |
- Cell Rep Med, 2024, S2666-3791(24)00201-5
- Biomed Pharmacother, 2024, 180:117468
- Transl Psychiatry, 2024, 14(1):166
|
|
S1035 |
Pazopanib HCl
|
Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death. |
- iScience, 2023, 26(7):107116
- NPJ Breast Cancer, 2022, 8(1):44
- J Pers Med, 2022, 12(2)258
|
|
S1189 |
Aprepitant
|
Aprepitant is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. Aprepitant inhibits HIV infection of human macrophages. |
- Br J Cancer, 2024, 10.1038/s41416-024-02608-8
- Inflammation, 2023, 46(1):256-269
- Nat Commun, 2022, 13(1):4995
|
|
S8401 |
Erdafitinib
|
Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis. |
- J Clin Invest, 2024, 134(2)e169241
- Adv Sci (Weinh), 2024, 11(16):e2303379
- Clin Cancer Res, 2024, 10.1158/1078-0432.CCR-24-1834
|
|
S1003 |
Linifanib (ABT-869)
|
Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3. |
- Cell Death Discov, 2023, 9(1):57
- Cell Death Discov, 2023, 9(1):57
- Cancer Cell, 2022, S1535-6108(22)00312-9
|
|
S7725 |
Sotuletinib (BLZ945)
|
Sotuletinib (BLZ945) 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.
|
- Nat Commun, 2024, 15(1):1987
- Immunity, 2023, 56(9):2152-2171.e13
- J Exp Med, 2023, 220(3)e20220857
|
|
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. |
- Sci Immunol, 2023, 10.1126/sciimmunol.adj5097
- J Nanobiotechnology, 2023, 21(1):44
- Brain Behav Immun, 2021, S0889-1591(21)00097-0
|
|
S1181 |
ENMD-2076
|
ENMD-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. |
- Cell, 2021, 184(2):334-351.e20
- Sci Adv, 2021, 7(4)eabd7851
- J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
|
|
S8874 |
PLX5622
|
PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3. |
- Pharmacol Res, 2023, 196:106912
- Cell Death Dis, 2023, 14(6):380
- Cell Death Dis, 2023, 14(6):380
|
|
S1220 |
OSI-930
|
OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1. |
- Nat Commun, 2024, 15(1):4739
- Cell Rep, 2019, 28(9):2331-2344
- Nat Biomed Eng, 2018, 2(8):578-588
|
|
S8015 |
Agerafenib (CEP-32496)
|
Agerafenib (CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2. |
- Mol Pharmacol, 2021, 99(6):435-447
- Dis Model Mech, 2020, dmm.047779
- Cancer Immunol Res, 2019,
|
|
S8721 |
PDGFR inhibitor 1
|
PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth. |
- Elife, 2023, 12e79840
- Elife, 2023, 12e79840
- Oncogene, 2022, 41(20):2860-2872
|
|
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. |
- Biomed Pharmacother, 2024, 180:117554
- J Exp Med, 2023, 220(3)e20220857
|
|
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. |
- Life (Basel), 2022, 12(10)1676
|
|
S8578 |
PRN1371
|
PRN1371 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.
|
- Int J Biol Sci, 2024, 20(9):3412-3425
- Nat Commun, 2021, 12(1):6572
|
|
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. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs. |
- Front Oncol, 2023, 13:1158857
|
|
E2629 |
Vimseltinib
|
Vimseltinib (DCC-3014) is a c-FMS (CSF-IR) and c-Kit dual inhibitor extracted from patent WO2014145025A2, Compound Example 10, has IC50s of <0.01 μM and 0.1-1 μM, respectively. |
|
|
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. |
- Cancer Immunol Immunother, 2024, 73(5):76
- Cancer Immunol Immunother, 2024, 73(5):76
|
|
S9620 |
Elzovantinib (TPX-0022)
|
Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models. |
|
|
S3523 |
AZD7507
|
AZD7507 is a potent and orally active CSF-1R inhibitor, with antitumor activity. |
|
|
E0616 |
Chiauranib
|
Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy. |
|
|
S3570 |
ARRY-382
|
ARRY-382 is a highly selective, oral inhibitor of the CSF1R with an IC50 of 9 nM. |
|
|
E1435New |
Tinengotinib
|
Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC). |
|
|
E1727New |
Pimicotinib
|
Pimicotinib (ABSK021) is an orally bioavailable inhibitor of colony stimulating factor 1 receptor (CSF1R). It enhances antitumor T-cell immune responses and inhibits the proliferation of tumor cells having potential immunomodulatory and antineoplastic activities. |
|
|