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

Sotuletinib hydrochloride  (Synonyms: BLZ945 hydrochloride)

Cat. No.: HY-12768A Purity: 99.43%
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Sotuletinib (BLZ945) hydrochloride 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 hydrochloride 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. : 2222138-31-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 36 publication(s) in Google Scholar

Other Forms of Sotuletinib hydrochloride:

Sotuletinib hydrochloride Related Antibodies

Top Publications Citing Use of Products

36 Publications Citing Use of MCE Sotuletinib hydrochloride

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

    Sotuletinib hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Sotuletinib (BLZ945) hydrochloride 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 hydrochloride can be used for microglia depletion, and for tumor and CNS-related disease research.[1].

    In Vitro

    Sotuletinib hydrochloride inhibits CSF-1-dependent proliferation (EC50=67 nM) in bone marrow-derived macrophages (BMDMs), and decreases CSF-1R phosphorylation, similar to CSF-1R antibody blockade. Sotuletinib hydrochloride also reduces viability of CRL-2467 microglia, Ink4a/Arf / BMDMs (PDG genetic background), and NOD/SCID BMDMs. Importantly, Sotuletinib hydrochloride 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 hydrochloride 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 hydrochloride Related Antibodies
    In Vivo

    Sotuletinib (2,000 ppm in diet, 21 days) hydrochloride 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) hydrochloride 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.
    Molecular Weight

    434.94

    Formula

    C20H23ClN4O3S
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (229.92 mM; Need ultrasonic)

    DMSO : 100 mg/mL (229.92 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 2.2992 mL 11.4958 mL 22.9917 mL
    5 mM 0.4598 mL 2.2992 mL 4.5983 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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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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    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: ≥ 2.5 mg/mL (5.75 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.75 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:  PBS

      Solubility: ≥ 10 mg/mL (22.99 mM); Suspended solution

    • Protocol 2

      Add each solvent one by one:  Saline

      Solubility: ≥ 10 mg/mL (22.99 mM); Clear solution

    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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation
    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.2992 mL 11.4958 mL 22.9917 mL 57.4792 mL
    5 mM 0.4598 mL 2.2992 mL 4.5983 mL 11.4958 mL
    10 mM 0.2299 mL 1.1496 mL 2.2992 mL 5.7479 mL
    15 mM 0.1533 mL 0.7664 mL 1.5328 mL 3.8319 mL
    20 mM 0.1150 mL 0.5748 mL 1.1496 mL 2.8740 mL
    25 mM 0.0920 mL 0.4598 mL 0.9197 mL 2.2992 mL
    30 mM 0.0766 mL 0.3832 mL 0.7664 mL 1.9160 mL
    40 mM 0.0575 mL 0.2874 mL 0.5748 mL 1.4370 mL
    50 mM 0.0460 mL 0.2299 mL 0.4598 mL 1.1496 mL
    60 mM 0.0383 mL 0.1916 mL 0.3832 mL 0.9580 mL
    80 mM 0.0287 mL 0.1437 mL 0.2874 mL 0.7185 mL
    100 mM 0.0230 mL 0.1150 mL 0.2299 mL 0.5748 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Sotuletinib hydrochloride Related Classifications

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    • 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:

    Sotuletinib2222138-31-8BLZ945BLZ 945BLZ-945c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RmicrogliatumorInhibitorinhibitorinhibit

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