Sotuletinib dihydrochloride
Based on 42 publication(s) in Google Scholar
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 2222138-40-9
- Formule: C20H24Cl2N4O3S
- Masse moléculaire:471.40
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Sotuletinib dihydrochloride
More- Cancer Cell. 2026 Jun 4:S1535-6108(26)00252-7. [Abstract]
- Nature. 2025 May;641(8064):1005-1016. [Abstract]
- Nature. 2025 Oct;646(8086):913-924. [Abstract]
- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Blood. 2019 Nov 28;134(22):1929-1940. [Abstract]
- Bioact Mater. 2022 Mar 11:16:107-119. [Abstract]
- Nat Neurosci. 2024 Aug;27(8):1522-1533. [Abstract]
- Adv Sci (Weinh). 2024 Dec;11(45):e2404756. [Abstract]
- Sci Adv. 2023 May 12;9(19):eade3559. [Abstract]
- Neuro Oncol. 2025 Feb 10;27(2):415-429. [Abstract]
- J Control Release. 2026 Mar 5:114797. [Abstract]
- Cell Death Dis. 2025 Oct 7;16(1):716. [Abstract]
- J Exp Med. 2023 Mar 6;220(3):e20220857. [Abstract]
- J Exp Med. 2020 Nov 2;217(11):e20191820. [Abstract]
- J Exp Med. 2016 Dec 12;213(13):2989-3005. [Abstract]
- J Neuroinflammation. 2024 Oct 3;21(1):248. [Abstract]
- Mol Ther. 2025 Nov 12:S1525-0016(25)00871-8. [Abstract]
- Adv Healthc Mater. 2024 Nov;13(28):e2401719. [Abstract]
- Clin Cancer Res. 2018 Mar 1;24(5):1176-1189. [Abstract]
- Acta Biomater. 2024 Jan 15:174:372-385. [Abstract]
- Acta Neuropathol. 2025 May 9;149(1):47. [Abstract]
- J Nucl Med. 2025 Feb 3;66(2):302-308. [Abstract]
- Proc Natl Acad Sci U S A. 2022 Oct 25;119(43):e2207280119. [Abstract]
- Cell Chem Biol. 2022 Jul 21;29(7):1113-1125.e6. [Abstract]
- Cancer Immunol Res. 2021 Jun;9(6):665-681. [Abstract]
- JCI Insight. 2025 Jan 9;10(1):e178146. [Abstract]
- CNS Neurosci Ther. 2026 Apr;32(4):e70857. [Abstract]
- Sci Rep. 2022 Nov 2;12(1):18521. [Abstract]
- Cell Signal. 2025 Mar:127:111550. [Abstract]
- Cancer Res Commun. 2024 Oct 1;4(10):2638-2652. [Abstract]
- Mol Immunol. 2026 Jul:195:93-100. [Abstract]
- Mol Carcinog. 2026 Jul;65(7):825-839. [Abstract]
- eNeuro. 2021 Mar 22;8(2):ENEURO.0318-20.2021. [Abstract]
- Anticancer Drugs. 2023 Oct 1;34(9):1035-1045. [Abstract]
- bioRxiv. 2026 Jun 18.
- bioRxiv. 2025 Oct 13.
- SSRN. 2025 Sep 25.
- bioRxiv. 2025 Jun 15.
- bioRxiv. 2025 May 1:2024.03.05.583602. [Abstract]
- Research Square Preprint. 2024 Dec 03.
- Res Sq. 2024 Nov 19.
- bioRxiv. 2024 July 16.
-
Cell Proliferation/Viability Assay
-
IHC
-
Apoptosis Analysis
-
In Vivo Efficacy Study
-
In Vivo Efficacy Study
Activité biologique
IC50: CSF1-R (1 nM)[1].
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.
Chemical Information
-
CAS No. 2222138-40-9
-
Masse moléculaire 471.40
-
Formule C20H24Cl2N4O3S
-
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
-
Synonyms
BLZ945 dihydrochloride
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (42)
-
Journal Impact Factor
-
Most Recent
-
Cancer Cell
Hypoxia shapes both therapeutic response and resistance in metastatic clear cell renal cell carcinoma. [Abstract]2026 Jun 4:S1535-6108(26)00252-7. PMID: 42242232 -
Nature
2025 May;641(8064):1005-1016. PMID: 40140584 -
Nature
2025 Oct;646(8086):913-924. PMID: 40769205 -
Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Blood
2019 Nov 28;134(22):1929-1940. PMID: 31697805 -
Bioact Mater
Remodeling tumor immunosuppressive microenvironment via a novel bioactive nanovaccines potentiates the efficacy of cancer immunotherapy. [Abstract]2022 Mar 11:16:107-119. PMID: 35386322
Sotuletinib dihydrochloride purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2022 Mar 11:16:107-119. [Abstract]
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.
-
Nat Neurosci
Spatiotemporally selective astrocytic ATP dynamics encode injury information sensed by microglia following brain injury in mice. [Abstract]2024 Aug;27(8):1522-1533. PMID: 38862791 -
Adv Sci (Weinh)
ASH1L in Hepatoma Cells and Hepatic Stellate Cells Promotes Fibrosis-Associated Hepatocellular Carcinoma by Modulating Tumor-Associated Macrophages. [Abstract]2024 Dec;11(45):e2404756. PMID: 39377228
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.
-
Sci Adv
2023 May 12;9(19):eade3559. PMID: 37172094 -
Neuro Oncol
Brain tumoroids: treatment prediction and drug development for brain tumors with fast, reproducible and easy-to-use personalized models. [Abstract]2025 Feb 10;27(2):415-429. PMID: 39252580 -
J Control Release
Ultrasound-guided nanocomposite hydrogel injection to enhance nerve repair via temporal delivery of a colony-stimulating factor 1 receptor inhibitor. [Abstract]2026 Mar 5:114797. PMID: 41794361 -
Cell Death Dis
E3 Ubiquitin ligases Cbl-b and c-Cbl maintain the homeostasis of macrophages by regulating the M-CSF/M-CSFR signaling axis. [Abstract]2025 Oct 7;16(1):716. PMID: 41057360 -
J Exp Med
2023 Mar 6;220(3):e20220857. PMID: 36584406
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).
-
J Exp Med
2020 Nov 2;217(11):e20191820. PMID: 32780802 -
J Exp Med
Modeling synovial sarcoma metastasis in the mouse: PI3'-lipid signaling and inflammation. [Abstract]2016 Dec 12;213(13):2989-3005. PMID: 27956588
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.
-
J Neuroinflammation
Tracking changes in functionality and morphology of repopulated microglia in young and old mice. [Abstract]2024 Oct 3;21(1):248. PMID: 39363245 -
Mol Ther
Microglia replacement by peripheral delivery of CSF1R inhibitor-resistant hematopoietic cells. [Abstract]2025 Nov 12:S1525-0016(25)00871-8. PMID: 41232525
Sotuletinib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Ther. 2025 Nov 12:S1525-0016(25)00871-8. [Abstract]
Survival curves of WT (black) and G793A (blue) BM macrophages treated for seven days with BLZ945 (Sotuletinib, 0.1-10000 nM).
-
Adv Healthc Mater
Paracrine Ovarian Cancer Cell-Derived CSF1 Signaling Regulates Macrophage Migration Dynamics in a 3D Microfluidic Model that Recapitulates In Vivo Infiltration Patterns in Patient-Derived Xenografts. [Abstract]2024 Nov;13(28):e2401719. PMID: 38807270 -
Clin Cancer Res
Dual Inhibition of PIK3C3 and FGFR as a New Therapeutic Approach to Treat Bladder Cancer. [Abstract]2018 Mar 1;24(5):1176-1189. PMID: 29222162 -
Acta Biomater
Spatial targeting of fibrosis-promoting macrophages with nanoscale metal-organic frameworks for idiopathic pulmonary fibrosis therapy. [Abstract]2024 Jan 15:174:372-385. PMID: 38072226 -
Acta Neuropathol
Multiplatform molecular analyses reveal two molecular subgroups of NF2-related schwannomatosis vestibular schwannomas with distinct tumour microenvironment and therapeutic vulnerabilities. [Abstract]2025 May 9;149(1):47. PMID: 40343504 -
J Nucl Med
First-in-Human Study of [11C]NCGG401 for Imaging Colony-Stimulating Factor 1 Receptors in the Brain. [Abstract]2025 Feb 3;66(2):302-308. PMID: 39746757 -
Proc Natl Acad Sci U S A
Endocytosis triggers V-ATPase-SYK-mediated priming of cGAS activation and innate immune response. [Abstract]2022 Oct 25;119(43):e2207280119. PMID: 36252040 -
Cell Chem Biol
Identifying enhancers of innate immune signaling as broad-spectrum antivirals active against emerging viruses. [Abstract]2022 Jul 21;29(7):1113-1125.e6. PMID: 35728599 -
Cancer Immunol Res
Chemotherapy Induces Tumor-Associated Macrophages that Aid Adaptive Immune Responses in Ovarian Cancer. [Abstract]2021 Jun;9(6):665-681. PMID: 33839687 -
JCI Insight
Sustained inhibition of CSF1R signaling augments antitumor immunity through inhibiting tumor-associated macrophages. [Abstract]2025 Jan 9;10(1):e178146. PMID: 39782686 -
CNS Neurosci Ther
Teriflunomide Attenuates Demyelination and Enhances Remyelination in Organotypic Brain Slice Cultures Through Modulation of Glial Cell Dynamics. [Abstract]2026 Apr;32(4):e70857. PMID: 41972458 -
Sci Rep
Long-term microglia depletion impairs synapse elimination and auditory brainstem function. [Abstract]2022 Nov 2;12(1):18521. PMID: 36323869 -
Cell Signal
Proguanil inhibits proliferation and migration in glioblastoma development through targeting CSF1R receptor. [Abstract]2025 Mar:127:111550. PMID: 39662608 -
Cancer Res Commun
Chemotherapy Enriches for Proinflammatory Macrophage Phenotypes that Support Cancer Stem-Like Cells and Disease Progression in Ovarian Cancer. [Abstract]2024 Oct 1;4(10):2638-2652. PMID: 39287565 -
Mol Immunol
CSF1R signaling contributes to macrophage-associated CCL11 production and eosinophil recruitment in murine allergic conjunctivitis. [Abstract]2026 Jul:195:93-100. PMID: 42105679 -
Mol Carcinog
RUNX1 Directly Activates WNT2 to Orchestrate Tumor-Associated Macrophage Reprogramming in Colorectal Cancer. [Abstract]2026 Jul;65(7):825-839. PMID: 41985081 -
eNeuro
Auditory Brainstem Deficits from Early Treatment with a CSF1R Inhibitor Largely Recover with Microglial Repopulation. [Abstract]2021 Mar 22;8(2):ENEURO.0318-20.2021. PMID: 33558268 -
Anticancer Drugs
Derazantinib, a fibroblast growth factor receptor inhibitor, inhibits colony-stimulating factor receptor-1 in macrophages and tumor cells and in combination with a murine programmed cell death ligand-1-antibody activates the immune environment of murine syngeneic tumor models. [Abstract]2023 Oct 1;34(9):1035-1045. PMID: 36729099 -
-
-
-
-
bioRxiv
Lipid Peroxidation and Type I Interferon Coupling Fuels Pathogenic Macrophage Activation Causing Tuberculosis Susceptibility. [Abstract]2025 May 1:2024.03.05.583602. PMID: 38496444 -
-
-
Pureté et documentation
Références
[1]. Pyonteck SM, et al. CSF-1R inhibition alters macrophage polarization and blocks glioma progression. Nat Med. 2013 Oct;19(10):1264-72. [Content Brief]
[2]. Pognan F, et al. Liver enzyme delayed clearance in rat treated by CSF1 receptor specific antagonist Sotuletinib. Curr Res Toxicol. 2022 Oct 29;3:100091. [Content Brief]
[3]. Chen Y, et al. Spatiotemporally selective astrocytic ATP dynamics encode injury information sensed by microglia following brain injury in mice. Nat Neurosci. 2024 Aug;27(8):1522-1533. [Content Brief]
[4]. Frosch M, et al. Microglia-neuron crosstalk through Hex-GM2-MGL2 maintains brain homeostasis. Nature. 2025 Oct;646(8086):913-924. [Content Brief]
[5]. Beckmann N, et al. Brain region-specific enhancement of remyelination and prevention of demyelination by the CSF1R kinase inhibitor BLZ945. Acta Neuropathol Commun. 2018 Feb 15;6(1):9. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)