BLZ945
For research use only.
Catalog No.S7725
16 publications
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.
3 Customer Reviews
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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.
Clin Cancer Res, 2017, 23(20):6021-6030. BLZ945 purchased from Selleck.
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Representative immunofluorescence staining and quantification of cleaved caspase 3 (CC3, red) in metastatic cancer cells (zsGreen) in livers of each treatment cohort. Nuclei were counterstained with DAPI (mean ± SEM).
Cancer Res, 2018, 78(15):4253-4269. BLZ945 purchased from Selleck.
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C, we evaluated the effects of CSF-1R inhibitor BLZ945 (500 nmol/L) or GW2580 (1 μmol/L) on the phenotypic changes of tumor-educated monocytes. D, the direct effects of BLZ945 on phenotypes of human primary monocytes were demonstrated. *, P < 0.05; **, P < 0.01; nonparametric Mann–Whitney U test. Each dot represented an individual experiment.
Clin Cancer Res, 2016, 22(15):3849-59.. BLZ945 purchased from Selleck.
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. | ||||||
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| 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] |
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| Assay |
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| 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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| Animal Research:[2] |
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Solubility (25°C)
| In vitro | DMSO | 79 mg/mL (198.25 mM) |
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| Ethanol | 3 mg/mL warmed (7.52 mM) | |
| Water | Insoluble | |
| 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 |
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| 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 |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| 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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
Does this molecule bind to any neurogenesis inhibiting enzymes? Which of the csf1r inhibitors is the most specific?
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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.
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Question 2:
We want to deliver the drug by oral gavage to mice, can you provide some advice about formulation?
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Answer:
S7725 BLZ945 can be dissolved in 0.5% CMC Na+1% Tween 80 at 20 mg/ml as a suspension.
