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BLZ945 (Sotuletinib)

Cat. No. M5316

All AbMole products are for research use only, cannot be used for human consumption.

BLZ945 (Sotuletinib) Structure
Synonym:

Sotuletinib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
1mg USD 35 In stock
2mg USD 55 In stock
5mg USD 85 In stock
10mg USD 125 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines TGCT cell
Preparation method TGCT cell pellets treated with sotuletinib at concentrations 0, 50, 250, and 500 µM for 96 h were subjected to check the expression of BAX and BCL‑2 by Western blot analysis.
Concentrations 0, 50, 250, and 500 µM
Incubation time 96 h
Animal Experiment
Animal models Female Balb/c SCID and C57BL/6 mice
Formulation 20% (v/v) 1,3-cyclodextrin
Dosages 100 mg/kg
Administration Oral
Chemical Information
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
References

[1] Mao Y, et al. Clin Cancer Res. Targeting Suppressive Myeloid Cells Potentiates Checkpoint Inhibitors to Control Spontaneous Neuroblastoma.

[2] Krauser JA, et al. Xenobiotica. Phenotypic and metabolic investigation of a CSF-1R kinase receptor inhibitor (BLZ945) and its pharmacologically active metabolite.

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Keywords: BLZ945 (Sotuletinib), Sotuletinib supplier, CSF-1R (c-Fms), inhibitors, activators

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