4- (2- (2- hydroxycyclohexylamino)benzothiazol- 6- yloxy)pyridine- 2- carboxylic acid methylamide

01/01/2016 - "To test the therapeutic efficacy of BLZ945 as a monotherapy or in combination with checkpoint inhibitors, we used a transgenic murine model (TH-MYCN) that develops aggressive spontaneous neuroblastoma. "
01/01/2016 - "In a transgenic mouse model (TH-MYCN) resembling high-risk human neuroblastoma, antagonizing CSF-1R with a selective inhibitor (BLZ945) modulates the induction of human and murine suppressive myeloid cells and efficiently limit tumor progression. "
01/01/2016 - "Although PD-1 blockade failed to control tumor growth in a transgenic murine neuroblastoma model, concurrent inhibition of colony stimulating factor 1 receptor (CSF-1R) by BLZ945 reprogrammed suppressive myeloid cells and significantly enhanced therapeutic effects. "
01/01/2018 - "However, when combined with cyclophosphamide plus topotecan, the CSF-1R inhibitor BLZ945, either without or with anti-human and anti-mouse CSF-1 mAbs, inhibited neuroblastoma growth and synergistically improved mouse survival. "

10/21/2020 - "In vivo studies showed that CA4-NPs induced enhanced distribution of BLZ945 in tumors, as the BLZ945 content was 3.75-fold in the CA4-NP + A15-BLZ-NP group compared to that of A15-BLZ-NP single treatment. "
01/01/2019 - "In present study, anti-tumor effects of combination treatment of BLZ945 and DTXL were investigated. "
05/01/2021 - "We demonstrate that a single systemic dose of D-BLZ targeted to TAMs decreases pro-tumor expression in TAMs and promotes cytotoxic T cell infiltration, resulting in prolonged survival and ameliorated disease burden compared to free BLZ945. "
01/01/2021 - "Meanwhile, such shrinkage also enables the rapid release of BLZ-945 in the perivascular regions of tumor to preferentially deplete TAMs (enriched in perivascular regions). "
10/21/2020 - "It is necessary to establish a tumor-targeting drug delivery system to reduce the off-target and side effects of BLZ945. "

01/01/2019 - "DTXL/BLZ945 combination treatment significantly inhibited tumor growth, reduced the abundance of TAMs, increased CD8+ T cell infiltration and prevented lung metastasis. "
10/01/2021 - "Here we demonstrate that targeting TAMs at distinct stages of the metastatic cascade using an inhibitor of colony-stimulating factor 1 receptor (CSF1R), BLZ945, in murine breast-to-brain metastasis models leads to antitumor responses in prevention and intervention preclinical trials. "
01/01/2019 - "We established a mouse ovarian cancer model and investigated the effect of BLZ945, DTXL single treatment or combination treatment on TAMs infiltration, tumor growth, CD8+ T cell infiltration and cancer metastasis. "

04/05/2023 - "In this study, a series of CB-NPs with different BLZ945/CA4 (B/C) ratios and drug loading contents were synthesized and evaluated on a hepatoma (H22) tumor-bearing mice model. "

05/01/2021 - "In this study, we present a novel hydroxyl dendrimer-mediated immunotherapy to deliver CSF-1R inhibitor BLZ945 (D-BLZ) from systemic administration selectively to TAMs in glioblastoma brain tumors to repolarize the tumor immune environment in a localized manner. "