BLZ945

For research use only.

Catalog No.S7725

19 publications

BLZ945 Chemical Structure

CAS No. 953769-46-5

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.

Selleck's BLZ945 has been cited by 19 publications

Purity & Quality Control

Choose Selective CSF-1R Inhibitors

Biological Activity

Description 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.
Targets
CSF-1R [1]
(Cell-free assay)
1 nM
In vitro

In bone marrow-derived macrophages (BMDMs), BLZ945 specifically inhibits CSF-1-dependent proliferation with EC50 of 67nM, and decreases CSF-1R phosphorylation. BLZ945 blocks the reciprocal effects between macrophages and glioma cells on the survival, proliferation and/ or polarization of each other to promote tumorigenesis. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse M-NFS-60 cells NGjufWlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MknGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCPLV7GV{03OCClZXzsd{Bp[XKkb4LpcochS1OIMTygSWM2OCB;IECuNFcyKM7:TT6= NEjRbI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK5N|AxOCd-MkmyPVMxODB:L3G+

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
pCSF1R / tCSF1R / pAKT / tAKT / p-mTOR / mTOR / pERK / ERK / p-NFKB / NFKB / p-P70S6K / P70S6K / Arg-1 ; 

PubMed: 30956894     


RAW264.7 macrophage cells were pre-treated with either BLZ945, PLX3397 or AK750 for 4h, and then washed with cold PBS to remove the drugs that are not internalized. After 7h or 48h of recovery in fresh medium, the cells were stimulated with either MCSF for 2h. The cells were then washed and analyzed for activation of signaling pathway by western blot.

30956894
In vivo In glioma-bearing mice, BLZ945 blocks tumor progression and significantly improves survival via CSF-1R inhibition. BLZ945 also inhibits orthotopic tumor growth of patient-derived proneural tumor spheres and cell lines in vivo. [1] BLZ945 (200 mg/kg, p.o.) decreases the growth of malignant cells in both mouse mammary tumor virus-driven polyomavirus middle T antigen (MMTV-PyMT) model of mammary carcinogenesis and keratin 14-expressing human papillomavirus type 16 (K14-HPV-16) transgenic model of cervical carcinogenesis. [2]

Protocol

Cell Research:[1]
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  • Cell lines: Glioma cell lines, BMDM, CRL-2467, HUVEC and HBMEC cell lines
  • Concentrations: ~6700 nM
  • Incubation Time: 96 hours
  • Method: Cell growth rate is determined using the MTT cell proliferation kit. Briefly, cells are plated in triplicate in 96-well plates: 1,000 cells per well for glioma cell lines, 5 x 1,000 cells per well for BMDM and CRL-2467, and 2.5 x 1,000 cells per well for HUVEC and HBMEC cell lines. For all experiments, media is changed every 48 h. Cells are grown in the presence or absence of 6.7–6,700 nM of BLZ945, or 8 μg/mL of CSF-1R neutralizing antibody. BMDM and CRL-2467 cells were supplemented with 10 ng/mL and 30 ng/ mL recombinant mouse CSF-1, respectively. Reduction of the MTT substrate is detected by colorimetric analysis using a plate reader as per the manufacturer’s protocol, and measured at 595 nm and 750 nm on a spectraMax 340pc plate reader.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Female MMTV-PyMT transgenic mice
  • Dosages: 200 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 79 mg/mL (198.25 mM)
Water Insoluble
Ethanol '3 mg/mL warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing. 		2.5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 398.48
Formula

C20H22N4O3S
CAS No. 953769-46-5
Storage powder
in solvent
Synonyms N/A
Smiles CNC(=O)C1=NC=CC(=C1)OC2=CC3=C(C=C2)N=C(S3)NC4CCCCC4O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04066244 Recruiting Drug: BLZ945 Amyotrophic Lateral Sclerosis Novartis Pharmaceuticals|Novartis December 30 2019 Phase 2
NCT02829723 Recruiting Drug: BLZ945|Drug: PDR001 Advanced Solid Tumors Novartis Pharmaceuticals|Novartis October 21 2016 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Does this molecule bind to any neurogenesis inhibiting enzymes? Which of the csf1r inhibitors is the most specific?

  • Answer:

    The IC50 of this compound to CSF1R is about 0.001uM, C-Kit 3.2uM and PDGFR-β 4.8uM. So it is relative specific to CSF1R.

  • Question 2:

    We want to deliver the drug by oral gavage to mice, can you provide some advice about formulation?

  • Answer:

    S7725 BLZ945 can be dissolved in 0.5% CMC Na+1% Tween 80 at 20 mg/ml as a suspension.

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CSF-1R Signaling Pathway Map
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID