BLZ945 - 10mM in DMSO, high purity , CAS No.953769-46-5(DMSO), Inhibitor of colony stimulating factor 1 receptor;Inhibitor of KIT proto-oncogene; receptor tyrosine kinase;Inhibitor of platelet derived growth factor receptor beta
BLZ945 - 10mM in DMSO, high purity , CAS No.953769-46-5(DMSO), Inhibitor of colony stimulating factor 1 receptor;Inhibitor of KIT proto-oncogene; receptor tyrosine kinase;Inhibitor of platelet derived growth factor receptor beta
BLZ945 is an orally active, potent and selective CSF-1R inhibitor with IC50 of 1 nM, >1000-fold selective against its closest receptor tyrosine kinase homologs.
Storage Temp
Store at -80°C
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of colony stimulating factor 1 receptor;Inhibitor of KIT proto-oncogene; receptor tyrosine kinase;Inhibitor of platelet derived growth factor receptor beta
Product Description
Information
BLZ945 BLZ945 is an orally active, potent and selective CSF-1R inhibitor with IC50 of 1 nM, >1000-fold selective against its closest receptor tyrosine kinase homologs. In vitro
In bone marrow-derived macrophages (BMDMs), BLZ945 specifically inhibits CSF-1-dependent proliferation with EC50 of 67nM, and decreases CSF-1R phosphorylation. BLZ945 blocks the reciprocal effects between macrophages and glioma cells on the survival, proliferation and/ or polarization of each other to promote tumorigenesis.
In vivo
In glioma-bearing mice, BLZ945 blocks tumor progression and significantly improves survival via CSF-1R inhibition. BLZ945 also inhibits orthotopic tumor growth of patient-derived proneural tumor spheres and cell lines in vivo. BLZ945 (200 mg/kg, p.o.) decreases the growth of malignant cells in both mouse mammary tumor virus-driven polyomavirus middle T antigen (MMTV-PyMT) model of mammary carcinogenesis and keratin 14-expressing human papillomavirus type 16 (K14-HPV-16) transgenic model of cervical carcinogenesis. Cell Data
