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

Sotuletinib dihydrochloride  (Synonyms: BLZ945 dihydrochloride)

Cat. No.: HY-12768B
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Sotuletinib (BLZ945) dihydrochloride 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 dihydrochloride 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. : 2222138-40-9

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Top Publications Citing Use of Products

36 Publications Citing Use of MCE Sotuletinib dihydrochloride

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

    Sotuletinib dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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.
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    Description

    Sotuletinib (BLZ945) dihydrochloride 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 dihydrochloride can be used for microglia depletion, and for tumor and CNS-related disease research[1][2][3][4].

    IC50 & Target

    IC50: CSF1-R (1 nM)[1].

    In Vivo

    Sotuletinib (2,000 ppm in diet, 21 days) dihydrochloride 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) dihydrochloride 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

    471.40

    Formula

    C20H24Cl2N4O3S

    CAS No.
    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Purity & Documentation
    References
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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.

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    Product Name:
    Sotuletinib dihydrochloride
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