2222138-40-9
Chemical Structure
Sotuletinib dihydrochloride
Synonym(s): BLZ945 dihydrochloride
- CAS No.: 2222138-40-9
- Formula:C20H24Cl2N4O3S
- Molecular Weight:471.40
IUPAC Name: 4-((2-(((1R,2R)-2-hydroxycyclohexyl)amino)benzo[d]thiazol-6-yl)oxy)-N-methylpicolinamide dihydrochloride
InChIKey: ZIHWHYXECXSBNA-LVVRIOTCSA-N
SMILES: O=C(C1=NC=CC(OC2=CC=C3N=C(N[C@H]4[C@H](O)CCCC4)SC3=C2)=C1)NC.[H]Cl.[H]Cl
Biological Activity: Sotuletinib (BLZ945) dihydrochloride is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib dihydrochloride can be used for microglia depletion, and for tumor and CNS-related disease research[1][2][3][4].
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Sotuletinib dihydrochloride | Sotuletinib (BLZ945) dihydrochloride is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib dihydrochloride can be used for microglia depletion, and for tumor and CNS-related disease research. | |||||||||||||||||||||
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References
- [1]. Pyonteck SM, et al. CSF-1R inhibition alters macrophage polarization and blocks glioma progression. Nat Med. 2013 Oct;19(10):1264-72. [Content Brief]
- [2]. Pognan F, et al. Liver enzyme delayed clearance in rat treated by CSF1 receptor specific antagonist Sotuletinib. Curr Res Toxicol. 2022 Oct 29;3:100091. [Content Brief]
- [3]. Chen Y, et al. Spatiotemporally selective astrocytic ATP dynamics encode injury information sensed by microglia following brain injury in mice. Nat Neurosci. 2024 Aug;27(8):1522-1533. [Content Brief]
- [4]. Frosch M, et al. Microglia-neuron crosstalk through Hex-GM2-MGL2 maintains brain homeostasis. Nature. 2025 Oct;646(8086):913-924. [Content Brief]
