A selective CSF1R inhibitor (IC50 = 1 nM) that inhibits CSF1-dependent proliferation (EC50 = 67 nM in bone marrow-derived macrophages); blocks tumor progression and significantly improves survival in glioma-bearing mice as well as in mouse models of breast and cervical cancer

BLZ-945 – 10 mg

Brand:
Cayman
CAS:
953769-46-5
Storage:
-20
UN-No:
Non-Hazardous - /

BLZ-945 is a selective inhibitor of the colony stimulating factor 1 receptor (CSF1R) with an IC50 value of 1 nM.{31423} It is more than 1,000-fold selective against its closest receptor tyrosine kinase homologs.{31423} It has been shown to inhibit CSF1-dependent proliferation with an EC50 value of 67 nM in bone marrow-derived macrophages.{31423} In glioma-bearing mice, CSF1R inhibition via BLZ-945 can block tumor progression and significantly improve survival.{31423} At 200 mg/kg, BLZ-945 decreased the growth of malignant cells in a mouse mammary tumor virus-driven polyomavirus middle T antigen model of mammary carcinogenesis and in a keratin 14-expressing human papillomavirus type 16 transgenic model of cervical carcinogenesis.{31424}  

 

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Description

A selective CSF1R inhibitor (IC50 = 1 nM) that inhibits CSF1-dependent proliferation (EC50 = 67 nM in bone marrow-derived macrophages); blocks tumor progression and significantly improves survival in glioma-bearing mice as well as in mouse models of breast and cervical cancer

Formal name: 4-[[2-[[(1R,2R)-2-hydroxycyclohexyl]amino]-6-benzothiazolyl]oxy]-N-methyl-2-pyridinecarboxamide

Synonyms: 

Molecular weight: 398.5

CAS: 953769-46-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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