2. Protein Tyrosine Kinase/RTK
  3. c-Fms
  4. Sotuletinib

BLZ945 est un CSF-1R (c-Fms) inhibiteur puissant, sélectif et cerveau-pénétrant avec un IC50 de 1 nM, montrant plus 1 000 fois de sélectivité par rapport à ses homologues récepteurs tyrosine kinase les plus proches.

Sotuletinib (BLZ945) is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib can be used for microglia depletion, and for tumor and CNS-related disease research.

For research use only. We do not sell to patients.

CAS No. : 953769-46-5

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Customer Review

Based on 36 publication(s) in Google Scholar

Other Forms of Sotuletinib:

Sotuletinib Related Antibodies

Top Publications Citing Use of Products

36 Publications Citing Use of MCE Sotuletinib

In Vivo Efficacy Study
IHC
Cell Proliferation/Viability Assay
Apoptosis Analysis
Histological Imaging/Staining

    Sotuletinib purchased from MedChemExpress. Usage Cited in: Mol Ther. 2025 Nov 12:S1525-0016(25)00871-8.

    Survival curves of WT (black) and G793A (blue) BM macrophages treated for seven days with BLZ945 (Sotuletinib, 0.1-10000 nM).

    Sotuletinib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Dec;11(45):e2404756.  [Abstract]

    Sotuletinib (BLZ945) (200 mg/kg; oral gavage; four times a week for 7 weeks) inhibited the infiltration of F4/80+ macrophages and reduced the expression of the M2 macrophage marker CD206 in DEN-CCl4-induced hepatocellular carcinoma-forming C57BL/6J mice.

    Sotuletinib purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2022 Mar 11:16:107-119.

    Prophylactic nanovaccine have a synergistic effect with BLZ-945 (Sotuletinib, 1 mg/kg; i.t.) and NLG-919 (2 mg/kg; i.t.), which inhibits tumor growth and prolongs survival in tumor-bearing mice.

    Sotuletinib purchased from MedChemExpress. Usage Cited in: J Exp Med. 2023 Mar 6;220(3):e20220857.  [Abstract]

    Quantification of iMG cell death by fluorescent Caspase 3/7 Dye for Apoptosis over 24 h in culture with complete medium treated with BLZ945 (Sotuletinib, 250 nM, 500 nM, or 1 µM; 5-20 h).

    Sotuletinib purchased from MedChemExpress. Usage Cited in: J Exp Med. 2016 Dec 12;213(13):2989-3005.  [Abstract]

    Graph of percent tumor growth over baseline for 21 d of treatment with or without 200 mg/kg of BLZ945 (Sotuletinib, oral gavage; once daily). *, P < 0.05; **, P < 0.01. n = 5 per group, Student’s t test.

    Sotuletinib purchased from MedChemExpress. Usage Cited in: J Exp Med. 2016 Dec 12;213(13):2989-3005.  [Abstract]

    Examples of photomicrographs of control tumors and BLZ945 (Sotuletinib, 200 mg/kg; oral gavage; once daily for 21 days)-treated tumors with corresponding GFP expression demonstrating the twofold increase in control tumor volume. Middle panel is control lungs with grossly visible metastases (arrowheads). Bars: (black) 10 µm; (white) 5 mm.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Sotuletinib (BLZ945) is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib can be used for microglia depletion, and for tumor and CNS-related disease research[1][2][3][4].

    IC50 & Target

    IC50: 1 nM (CSF-1R), 3.2 μM (c-Kit), 4.8 μM (PDGFRβ), 9.1 μM (Flt3)[1]
    Cellular Effect
    Cell Line Type Value Description References
    CT26 IC50
    1 nM
    Compound: BLZ945
    Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 6 days by MTT assay
    Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 6 days by MTT assay
    		[PMID: 36335744]
    NFS-60 EC50
    71 nM
    Compound: 10; BLZ945
    Antiproliferative activity against mouse M-NFS-60 cells harboring CSF1
    Antiproliferative activity against mouse M-NFS-60 cells harboring CSF1
    		[PMID: 29293000]
    Panc02 IC50
    18 μM
    Compound: BLZ945
    Antitumour activity against mouse Panc02 cells implanted in po dosed C57BL/6 mouse assessed as reduction in EMR1 F4/80 mRNA expression after 5 days
    Antitumour activity against mouse Panc02 cells implanted in po dosed C57BL/6 mouse assessed as reduction in EMR1 F4/80 mRNA expression after 5 days
    		[PMID: 32787110]
    Panc02 IC50
    56 μM
    Compound: BLZ945
    Antitumour activity against mouse Panc02 cells implanted in po dosed C57BL/6 mouse assessed as reduction in CD4 mRNA expression after 5 days
    Antitumour activity against mouse Panc02 cells implanted in po dosed C57BL/6 mouse assessed as reduction in CD4 mRNA expression after 5 days
    		[PMID: 32787110]
    In Vitro

    Treatment of bone marrow-derived macrophages (BMDMs) with Sotuletinib inhibits CSF-1-dependent proliferation (EC50=67 nM), and decreases CSF-1R phosphorylation, similar to CSF-1R antibody blockade. Sotuletinib also reduces viability of CRL-2467 microglia, Ink4a/Arf / BMDMs (PDG genetic background), and NOD/SCID BMDMs. Importantly, Sotuletinib treatment in culture does not affect proliferation of any PDG-derived tumor cell lines (all Csf-1r-negative), or U-87 MG human glioma cells, and PDG cell tumor sphere formation is unaffected. Thus, Sotuletinib has no direct effects on glioma cells, and perturbs macrophage survival through CSF-1R inhibition[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Sotuletinib Related Antibodies
    In Vivo

    Sotuletinib (2,000 ppm in diet, 21 days) depletes more than 90% of microglia in C57BL6/J mice[3].
    Sotuletinib hydrochloride (200 mg/kg, p.o., 7 days) depletes more than 90% microglia in C57BL6/J mice, and subsequntenly used for microglia replacement[4].
    Sotuletinib (60-169 mg/kg, p.o., 5 days) dose- and time-dependently depletes microglia in C57BL6/J mice, and newly generated microglia after BLZ945 removal reached normal levels 3 days after last dose[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    398.48

    Formula

    C20H22N4O3S
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light brown

    SMILES

    O=C(C1=NC=CC(OC2=CC=C3N=C(N[C@H]4[C@H](O)CCCC4)SC3=C2)=C1)NC
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 83.33 mg/mL (209.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5095 mL 12.5477 mL 25.0954 mL
    5 mM 0.5019 mL 2.5095 mL 5.0191 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  20% SBE-β-CD in Saline

      Solubility: 10 mg/mL (25.10 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/0.1% Tween-80 in Saline water

      Solubility: 20 mg/mL (50.19 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.97%

    SDS (538 KB)

    COA (247 KB) HNMR (144 KB) RP-HPLC (162 KB) LCMS (235 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Cell growth rate is determined using the MTT cell proliferation kit. Briefly, cells are plated in triplicate in 96-well plates: 1×103 cells per well for glioma cell lines, 5×103 cells per well for BMDM and CRL-2467, and 2.5×103 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 Sotuletinib, or 8 μg/mL of CSF-1R neutralizing antibody. To test the sensitivity to PDGFR inhibition, PDGC lines are cultured in the presence of 10,000 nM STI571 or 10,000 nM PTK787 (diluted from 10 mM stock solutions in DMSO). HUVEC and HBMEC cells are supplemented with ECGF supplied by the manufacturer unless otherwise indicated. Reduction of the MTT substrate is detected by colorimetric analysis using a plate reader as per the manufacturer’s protocol. 10 μL of MTT labeling reagent is added to each well and then incubated for 4 h at 37°C, followed by the addition of 100 μL MTT solubilization reagent overnight. The mixture is gently resuspended and absorbance is measured at 595 nm and 750 nm on a spectraMax 340pc plate reader[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    Tumors are measured using calipers and volumes calculated based on the formula: volume=(width)2×length/2. In MMTV-PyMT mouse studies, 56-63 d old female mice are randomized into groups based on tumor volumes and dosed with either 20% Captisol vehicle or 200 mg/kg Sotuletinib. Dosing is administered by oral gavage once daily and tumor volumes are measured twice weekly. 5A1 rat anti-mouse CSF1 neutralizing antibody or rat IgG control is dosed at 10 mg/kg by intraperitoneal injection every 5 d. To calculate pulmonary metastasis in MMTV-PyMT transgenic mice, formalin-fixed paraffin-embedded lungs are serially sectioned and stained with hematoxylin and eosin. Tumor regions are scored by tumor burden (total tumor area divided by total lung area), size (tumor diameter), and according to the total number of individual metastases counted in a single-blind fashion. These values are averaged across the entire depth of the lung to obtain the final value.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5095 mL 12.5477 mL 25.0954 mL 62.7384 mL
    5 mM 0.5019 mL 2.5095 mL 5.0191 mL 12.5477 mL
    10 mM 0.2510 mL 1.2548 mL 2.5095 mL 6.2738 mL
    15 mM 0.1673 mL 0.8365 mL 1.6730 mL 4.1826 mL
    20 mM 0.1255 mL 0.6274 mL 1.2548 mL 3.1369 mL
    25 mM 0.1004 mL 0.5019 mL 1.0038 mL 2.5095 mL
    30 mM 0.0837 mL 0.4183 mL 0.8365 mL 2.0913 mL
    40 mM 0.0627 mL 0.3137 mL 0.6274 mL 1.5685 mL
    50 mM 0.0502 mL 0.2510 mL 0.5019 mL 1.2548 mL
    60 mM 0.0418 mL 0.2091 mL 0.4183 mL 1.0456 mL
    80 mM 0.0314 mL 0.1568 mL 0.3137 mL 0.7842 mL
    100 mM 0.0251 mL 0.1255 mL 0.2510 mL 0.6274 mL
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    Sotuletinib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Sotuletinib953769-46-5BLZ945BLZ 945BLZ-945c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RmicroglialInhibitorinhibitorinhibit

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