Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
2.5095 mL
12.5477 mL
25.0954 mL
5 mM
0.5019 mL
2.5095 mL
5.0191 mL
10 mM
0.2510 mL
1.2548 mL
2.5095 mL
50 mM
0.0502 mL
0.2510 mL
0.5019 mL
Description
BLZ945(Sotuletinib) is an orally active, potent and selective inhibitor with of 1 nM, >1000-fold selective against its closest receptor tyrosine kinase homologs.
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.
