[CAS NO. 953769-46-5] BLZ945
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PRODUCTS SPECIFICATIONS [953769-46-5]
Catalog
SLK-S7725
Brand
Selleck
CAS
953769-46-5
DESCRIPTION [953769-46-5]
Overview
| MDL | MFCD28142668 |
|---|---|
| Molecular Weight | 398.48 |
| Molecular Formula | C20H22N4O3S |
| SMILES | O=C(NC)C1=NC=CC(OC2=CC=C3N=C(N[C@H]4[C@H](O)CCCC4)SC3=C2)=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
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.
Targets
| CSF-1R [1] (Cell-free assay) |
| 1 nM |
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.
References
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