In vitro: In bone marrow-derived macrophages (BMDMs), Sotuletinib (BLZ945) specifically inhibits CSF-1-dependent proliferation with EC50 of 67nM, and decreases CSF-1R phosphorylation. Sotuletinib (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. Sotuletinib (BLZ945) also inhibits orthotopic tumor growth of patient-derived proneural tumor spheres and cell lines in vivo. Sotuletinib (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.
Kidney Int. 2023 Jul;104(1):108-123.
Single cell landscape of parietal epithelial cells in healthy and diseased states
BLZ945 (Sotuletinib) purchased from AbMole
Res Sq. 2023 Jun 6;rs.3.rs-2972427.
CAR T-cell design dependent remodeling of the brain tumor immune microenvironment identify macrophages as key players that inhibit or promote anti-tumor activity
BLZ945 (Sotuletinib) purchased from AbMole
| Molecular Weight | 398.48 |
| Formula | C20H22N4O3S |
| CAS Number | 953769-46-5 |
| Solubility (25°C) | DMSO 69 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related CSF-1R (c-Fms) Products |
|---|
| Tinengotinib
Tinengotinib is a modulator of several protein kinases, such as Aurora kinase, VEGFR kinase, and CSF-1R, etc. Tinengotinib can be used in studies related to diseases mediated by abnormalities in these kinases. |
| AMG-820
AMG-820 is an anti-colony stimulating factor 1 receptor (CSF1R) monoclonal antibody. |
| CSF1R-IN-15
CSF1R-IN-15 is an inhibitor targeting CSF1R. |
| Pimicotinib
Pimicotinib is a novel, orally bioavailable, highly selective small-molecule inhibitor of colony-stimulating factor 1 (CSF-1) with antitumor activity and less inhibitory effects on c-Kit and PDGFR. |
| c-Fms-IN-14
c-Fms-IN-14 is a c-Fms inhibitor with an IC50 value of 4 nM. |
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