| Identification | Back Directory | [Name]
Glutaminase-IN-1 | [CAS]
2247127-79-1 | [Synonyms]
Glutamise-IN-1
Glutaminase-IN-1
CB839 derivative
Glutaminase inhibitor 1
GlutaminaseIN1,Glutaminase IN 1
2-Pyridineacetamide, N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-selenadiazol-2-yl]- | [Molecular Formula]
C26H24F3N7O3Se | [MDL Number]
MFCD31807665 | [MOL File]
2247127-79-1.mol | [Molecular Weight]
618.47 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (202.11 mM) | [form ]
Solid | [pka]
11.56±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity. | [in vivo]
Glutaminase-IN-1(10 mg/kg, s.c.) reduced the size and weight of the HCT116 tumor, and statistical analysis showed that the 40% reduction in tumor weight by CPD20 is statistically significant. Glutaminase-IN-1 could statistically significantly prolong the survival of H22-bearing mice[1]. | [References]
[1] Chen Z, et al. Novel 1,3,4-Selenadiazole Containing Kidney-Type Glutaminase Inhibitors Showed Improved Cellular Uptake and Antitumor Activity. J Med Chem. 2018 Dec 13. DOI:10.1021/acs.jmedchem.8b01198 |
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