Sotuletinib (BLZ945) is an orally active, potent and selective CSF-1R inhibitor with an IC50 of 1 nM, which is more than 1000-fold more selective than its closest receptor tyrosine kinase homolog.

 

Brand: BCM

 

Target: c-Fms; CSF-1R

 

Signaling Pathways: Tyrosine Kinase/Adaptors

 

In Vitro: In bone marrow-derived macrophages (BMDMs), BLZ945 specifically inhibits CSF-1-dependent proliferation with EC50 of 67 nM, and decreases CSF-1R phosphorylation. 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. BLZ945 also inhibits orthotopic tumor growth of patient-derived proneural tumor spheres and cell lines in vivo. 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.

 

pKa: 13.92±0.46(Predicted)

 

Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.

 

Isomeric SMILES: CNC(=O)C1=NC=CC(=C1)OC2=CC3=C(C=C2)N=C(S3)N[C@@H]4CCCC[C@H]4O  

 

InChIKey: ADZBMFGQQWPHMJ-RHSMWYFYSA-N  

 

InChI: 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

 

Attribute
[Chem Name]	4-[[2-[[(1R,2R)-2-hydroxycyclohexyl]amino]-1,3-benzothiazol-6-yl]oxy]-N-methylpyridine-2-carboxamide
[Synonym]	Sotuletinib; BLZ945; BLZ-945
[CAS No.]	953769-46-5
[MDL No.]	MFCD28142668
[Formula]	C20H22N4O3S
[Molecular]	398.48
[Form]	Pale yellow solid
[Storage]	Keep in dark place. Sealed in dry, 2-8°C

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