| Identification | Back Directory | [Name]
SN-32976 | [CAS]
1246202-11-8 | [Synonyms]
SN-32976
Ethanamine, 2-[[4-[4-[2-(difluoromethyl)-4-methoxy-1H-benzimidazol-1-yl]-6-(4-morpholinyl)-1,3,5-triazin-2-yl]-1-piperazinyl]sulfonyl]-N,N-dimethyl- | [Molecular Formula]
C24H33F2N9O4S | [MOL File]
1246202-11-8.mol | [Molecular Weight]
581.64 |
| Hazard Information | Back Directory | [Description]
SN32976 is a novel potent pi3kα inhibitor | [Uses]
SN32976 is a potent and selective class I PI3K and mTOR inhibitor with IC50s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects[1]. | [in vivo]
SN32976 (37.5-75 mg/kg; po; daily; for 21 days) inhibits tumor growth in U-87 MG tumor xenograft models[1]. | Animal Model: | 6-8 week old female balb/c nude or female balb/c Rag1?/? mice inoculated with U-87 MG cells[1] | | Dosage: | 37.5 mg/kg; 75 mg/kg | | Administration: | po; daily; for 21 days | | Result: | Inhibited tumor growth in U-87 MG tumor xenograft models.
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| [IC 50]
PI3Kα: 15.1 nM (IC50); PI3Kβ: 461 nM (IC50); PI3Kγ: 110 nM (IC50); PI3Kδ: 134 nM (IC50); mTOR: 194 nM (IC50) | [References]
[1] Gordon W Rewcastle, et al. Biological characterization of SN32976, a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors. Oncotarget. 2017 Jul 18;8(29):47725-47740. DOI:10.18632/oncotarget.17730 |
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