BLZ-945

BLZ-945 is a selective inhibitor of the colony stimulating factor 1 receptor (CSF1R) with an IC50 value of 1 nM. It is more than 1,000-fold selective against its closest receptor tyrosine kinase homologs. It has been shown to inhibit CSF1-dependent proliferation with an EC50 value of 67 nM in bone marrow-derived macrophages. In glioma-bearing mice, CSF1R inhibition via BLZ-945 can block tumor progression and significantly improve survival. 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.Formal Name: 4-[[2-[[(1R,2R)-2-hydroxycyclohexyl]amino]-6-benzothiazolyl]oxy]-N-methyl-2-pyridinecarboxamide. CAS Number: 953769-46-5. Molecular Formula: C20H22N4O3S. Formula Weight: 398.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/mL, DMF:PBS (pH 7.2) (1:8): 0.1 mg/mL, DMSO: 15 mg/mL, Ethanol: 1 mg/mL. lambdamax: 229, 273 nm. SMILES: O=C(NC)C1=CC(OC2=CC(SC(N[C@@H]3CCCC[C@H]3O)=N4)=C4C=C2)=CC=N1. InChi Code: InChI=1S/C20H22N4O3S/c1-21-19(26)16-10-13(8-9-22-16)27-12-6-7-15-18(11-12)28-20(24-15)23-14-4-2-3-5-17(14)25/h6-11,14,17,25H,2-5H2,1H3,(H,21,26)(H,23,24)/t14-,17-/m1/s1. InChi Key: ADZBMFGQQWPHMJ-RHSMWYFYSA-N.