c-Fms Inhibitor

CSF1R-IN-15 (compound 23) is an inhibitor targeting CSF1R. The colony-stimulating factor-1 receptor (CSF1R) is a tyrosine kinase embedded in the cell membrane of macrophages. The receptor is activated by colony-stimulating factor-1 (CSF-1) and interleukin-34, and signaling via CSF1R is crucial for the differentiation, proliferation, and survival of macrophages.

c-Fms-IN-7 is a cFMS inhibitor extracted from patent WO2011079076A1, example159, has an IC₅₀ of 18.5 nM.

c-Fms-IN-14 (Example 76) is a c-Fms inhibitor with an IC₅₀ value of 4 nM. c-Fms-IN-14 can be used for research of cancer and autoimmune diseases.

The Anti-CSF2/GM-CSF Antibody is a CHO-expressed human antibody that targets CSF2/GM-CSF. The Anti-CSF2/GM-CSF Antibody has a huIgG1-type heavy chain and a huλ-type light chain, with a predicted molecular weight (MW) of 145.02 kDa. The isotype control for the Anti-CSF2/GM-CSF Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).

NPA101.3 is an orally active RET receptor tyrosine kinase and VEGFR2 inhibitor (RET IC₅₀ = 0.001 μM, RET^V804M IC₅₀ = 0.008 μM, VEGFR2 IC₅₀ = 0.003 μM). NPA101.3 inhibits purified TRKA (IC₅₀ = 32 nM) and CSF1R (IC₅₀ = 46 nM). NPA101.3 completely suppresses tumor formation in RET^/C634Y-transformed cells and also attenuates tumor formation in HRAS^/G12V-transformed cells. NPA101.3 can be used in the research of RET-driven cancers.

Antifibrotic agent 1 is an orally active anti-idiopathic pulmonary fibrosis (IPF) agent. Antifibrotic agent 1 effectively attenuates IPF-related processes, including TGF-β induced EMT and FMT processes, as well as pro-fibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α and Src family kinases (SFKs), while sparing VEGFRs, FGFRs and Abl to minimize off-target toxicity. Antifibrotic agent 1 has potent anti-fibrotic activity in Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis mice model.

ELB041 (AFS98) is a rat monoclonal anti-murine c-fms antibody (IgG2a). AFS98 inhibits M-CSF–dependent colony formation and cell growth by blocking the binding of M-CSF to its receptor. AFS98 prevents development of fatty streaks in ApoE-deficient mice. ELB041 can be used for the research of atherosclerosis.

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC₅₀ values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies.

Pazopanib (Hydrochloride) (Standard) is the analytical standard of Pazopanib (Hydrochloride). This product is intended for research and analytical applications. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

PRN1371 (Standard) is the analytical standard of PRN1371 (HY-101768). This product is intended for research and analytical applications. PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC₅₀s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively.

OSI-930 (Standard) is the analytical standard of OSI-930 (HY-10204). This product is intended for research and analytical applications. OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC₅₀s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity.

Dovitinib (Standard) is the analytical standard of Dovitinib. This product is intended for research and analytical applications. Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity.

SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC₅₀ values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC₅₀ values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer.

PLX5622 (Standard) is the analytical standard of PLX5622 (HY-114153). This product is intended for research and analytical applications. PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC₅₀=0.016 μM; K_i=5.9 nM). PLX5622 allows for extended and specific microglial cells elimination, preceding and during pathology development. PLX5622 is an ideal choose for microglia function research in healthy or diseased states. PLX5622 has been verified by MedChemExpress, which demonstrates desirable microglia depletion efficiency in mice. PLX5622 is predominantly administered via ad libitum diets with a dose of 1200 ppm.

Pexidartinib (Standard) is the analytical standard of Pexidartinib. This product is intended for research and analytical applications. Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity.

Elzovantinib (Standard) is the analytical standard of Elzovantinib (HY-111787). This product is intended for research and analytical applications. Elzovantinib (TPX-0022) is an oral-active inhibitor of SRC, MET and c-FMS, with IC₅₀ values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.

Anti-CSF1R/CD115 Antibody (2-4A5-4) is a kind of rat IgG1 κ chimeric antibody inhibitor, targeting to human CSF1R/CD115. Anti-CSF1R/CD115 Antibody (2-4A5-4) can neutralize colony stimulating factor 1 receptor (CSF1R), also known as CD115. Anti-CSF1R/CD115 Antibody (2-4A5-4) can be used for the detections of immunohistochemistry, functional assays and flow cytometry.

PF 477736 (Standard) is the analytical standard of PF 477736 (HY-10032). This product is intended for research and analytical applications. PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.

CSF1R-IN-1 (Standard) is the analytical standard of CSF1R-IN-1 (HY-101774). This product is intended for research and analytical applications. CSF1R-IN-1 is a CSF1R inhibitor with an with an IC₅₀ of 0.5 nM.

Linifanib (Standard) is the analytical standard of Linifanib. This product is intended for research and analytical applications. Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.