c-fms

c-Fms-IN-1 is an inhibitor of c-FMS kinase (IC50 = 0.8 nM).

c-Fms-IN-2 is an inhibitor of c-FMS kinase (IC50 = 24 nM).

c-Fms-IN-3 is a novel inhibitor of c-FMS, suitable for research on antirheumatic and anti-inflammatory diseases.

c-Fms-IN-13 (compound 14) is a potent FMS kinase inhibitor (IC50 = 17 nM) and serves as an anti-inflammatory agent.

c-Fms-IN-9 is a c-FMS inhibitor that inhibits unphosphorylated c-FMS kinase (uFMS) and uKIT with IC50 values of <0.01 μM and 0.1-1 μM, respectively.

c-Fms-IN-8 is a colony-stimulating factor-1 receptor (CSF-1R, c-FMS) Type II inhibitor (IC50: 9.1 nM). It is compound 4a in the reference.

c-Fms-IN-10, a derivative of thieno [3,2-d] pyrimidine, is a kinase inhibitor of FMS (Colony-stimulating factor-1 receptor, CSF-1R; IC50: 2 nM) with anti-tumor activity.

c-Fms-IN-12 is an FMS kinase inhibitor that also inhibits c-KIT and induces apoptosis in A549 cells. c-Fms-IN-12 is a potential broad-spectrum anti-cancer agent that has demonstrated therapeutic effects in a variety of cancer types.

c-Fms-IN-14 (Example 76) is a potent c-Fms kinase inhibitor with an IC50 of 4 nM, used in cancer and autoimmune disease research [1].

c-Fms-IN-6 is a potent inhibitor of c-FMS (IC50 ≤10 nM for unphosphorylated c-FMS) and weakly inhibits unphosphorylated c-KIT and PDGFR (IC50: >1 μM).

c-Fms-IN-7 is a cFMS inhibitor with an IC50 of 18.5 nM.

Edicotinib (JNJ-527) is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment.

Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035 1.3 4.6 7 11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.

Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms (IC50=10 30 47 84 74 140 146 nM). Pazopanib has antitumor activity.

Pazopanib Hydrochloride (Votrient 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.

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

GW 5074 (Raf1 Kinase Inhibitor I)(IC50=9 nM) is an effective and specific c-Raf inhibitor. It has no effect on the activities of JNK1 2 3, MEK1, MKK6 7, CDK1 2, c-Src, p38 MAP, VEGFR2 or c-Fms.

AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.

OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.

PLX5622 is a highly selective, brain-penetrant, and orally active CSF1R inhibitor.

JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1 2 4 inhibitor (IC50: 4.7 18.7 1 nM) with over 10-fold selectivity compared to MNK2 and Fms, and no inhibition of Met, c-Kit, or PDGFRβ in the A375 cell line.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

Sotuletinib (BLZ945) is an orally active, effective and specific CSF-1R inhibitor (IC50: 1 nM), >1000-fold selective against its closest receptor tyrosine kinase homologs.

Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.

KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.

SNS-314 Mesylate (SNS-314) is an effective and specific Aurora A/B/C inhibitor (IC50: 9/31/3 nM). It is less inhibition of Trk A/B, Fms, Flt4, c-Raf, Axl, and DDR2.

cFMS Receptor Inhibitor II is a CSF1R kinase (FMS Receptor; colony stimulating factor 1 receptor; Macrophage colony-stimulating factor receptor) inhibitor with an IC50 of 2.8 nM, demonstrating significant selectivity over other kinases. This compound also exhibits notable CSF1R inhibition with an IC50 of 1.4 μM in cellular assays.

Ki-20227 is a specific c-Fms tyrosine kinase(CSF1R) inhibitor (IC50: 2 nM). It also has certain inhibitory against VEGFR2(IC50: 12 nM) and c-Kit PDGFRβ(IC50: 451 217 nM), respectively.

AZD7507 is a CSF-1R inhibitor with an IC50 of 32 nM. AZD7507 has antitumor activity.

AEE788 (NVP-AEE 788) has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.

CSF1R-IN-1 is a CSF1R inhibitor with an IC50 of 0.5 nM.

Dovitinib (CHIR-258) (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3 c-Kit, IC50: 1 2 nM), also effective to class IV (FGFR1 3) and class V (VEGFR1-4) RTKs (IC50: 8-13 nM), less potent to EGFR, InsR, EphA2, c-Met, IGF-1R, Tie2, and HER2.

PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6 1.3 4.1 19.3 8.1 nM for FGFR1 2 3 4 and CSF1R).

Tyrphostin AG1296 (Tyrphostin AG 1296) is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.

BIX02189 is a potent and selective inhibitor of MEK5 and ERK5 (IC50: 1.5 nM and 59 nM).

Altiratinib (DCC-2701)(DCC-2701) is a novel c-MET/TIE-2/VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with an HGF antagonist in vitro.

AZD2932 is a potent, multi-targeted kinase inhibitor of VEGFR2, PDGFβ, Flt-3, and c-Kit.

HPK1-IN-7 is an orally active HPK1 inhibitor. It shows selectivity against IRAK4 (59 nM) and GLK (140 nM).

SKLB4771 (FLT3-IN-1) is a novel potent and selective Flt3 inhibitor.

Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.

Linifanib (AL-39324) (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).

CSF1R-IN-2 is an oral-active SRC, MET and c-FMS inhibitor (IC50s: 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively).

Vimseltinib (DCC-3014) is a dual inhibitor targeting c-FMS (CSF-IR) and c-Kit with IC50 values of less than 0.01 μM and 0.1-1 μM, respectively.

BIX02188 is a selective and potent MEK5 inhibitor that inhibits MEK5-induced apoptosis in cells expressing the oncogenic mutant FLT3-ITD.

AC710 is a potent PDGFR inhibitor with Kds of 0.6 nM for FLT3, 1 nM for KIT, 1.57 nM for CSF1R, 1.3 nM for PDGFRα, and 1 nM for PDGFRβ.

Lestaurtinib (CEP 701) is an orally available and selective inhibitor of FMS-like tyrosine kinase-3 (FLT3, IC50: 0.9 nM), which inhibits FLT3 autophosphorylation in vitro.Lestaurtinib promotes the expression of c-MYC, inhibits the phosphorylation of RPTKs, and has high affinity for TrkA and JAK2. Lestaurtinib promotes c-MYC expression, inhibits phosphorylation of RPTKs, has a high affinity for TrkA and JAK2, induces apoptosis and cell growth arrest, and can be used to study leukemia.

GTP-14564 is a novel tyrosine kinase inhibitor that also inhibits wt-FLT3 and ITD-FLT3. GTP-14564 inhibits the growth of interleukin-3-independent Ba/F1 expressing ITD-FLT3 at 3 μ m, whereas a 30-fold higher concentration of GTP-14564 is required to inhibit the FLT3 ligand-dependent growth (wt-FLT3) of Ba/F3 expressing wild-type FLT3. F3 expressing wild-type FLT3 (wt-FLT3).

Dovitinib lactate (TKI-258 lactate)(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).

PKC412(Midostaurin (PKC412); CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.