4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide
4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide Basic information
- Product Name:
- 4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide
- Synonyms:
-
- 4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide
- BLZ945
- 4-[[2-[[(1R,2R)-2-hydroxycyclohexyl]amino]-1,3-benzothiazol-6-yl]oxy]-N-methylpyridine-2-carboxamide
- 106245
- BLZ-945;BLZ 945
- CS-1735
- 4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide BLZ945
- 4-[[2-[[(1R,2R)-2-Hydroxycyclohexyl]amino]-6-benzothiazolyl]oxy]-N-methyl-2-pyridinecarboxamide
- CAS:
- 953769-46-5
- MF:
- C20H22N4O3S
- MW:
- 398.48
- Product Categories:
-
- API
- Inhibitors
- Mol File:
- 953769-46-5.mol
4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide Chemical Properties
- Density
- 1.377±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in EtOH; insoluble in H2O; ≥19.9 mg/mL in DMSO
- form
- solid
- pka
- 13.92±0.46(Predicted)
- color
- Pale yellow
- InChIKey
- ADZBMFGQQWPHMJ-RHSMWYFYSA-N
- SMILES
- C1(C(NC)=O)=NC=CC(OC2C=C3SC(N[C@@H]4CCCC[C@H]4O)=NC3=CC=2)=C1
4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide Usage And Synthesis
Uses
BLZ945 is a tumor-associated macrophage targeting the treatment of glioblastoma multiforme, a most common type of aggresive brain cancer.
in vivo
Mice are treated with Sotuletinib or vehicle, and evaluated for symptom-free survival. Median survival in the vehicle-treated cohort is 5.7 weeks. In striking contrast, Sotuletinib significantly improves long-term survival. This endpoint is chosen because Ink4a/Arf / mice develop spontaneous tumors, including lymphomas and sarcomas, beginning at ~30 weeks. Sotuletinib is well-tolerated over long-term treatment, with no visible side-effects, consistent with histopathological studies. Histological grading revealed high-grade, invasive gliomas in all vehicle-treated mice. By contrast, Sotuletinib-treated animals have significantly less-malignant tumors, and no detectable lesions in 55.6% of asymptomatic mice at the endpoint[1]. Mice receiving Sotuletinib shows reduced CSF1R staining in both cervical tumors and the associated stroma, with a significant decrease in CSF1R+ stromal macrophages relative to vehicle-treated mice (P<0.05)[2].
storage
+4°C
4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMideSupplier
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