| Identification | Back Directory | [Name]
GLS1 Inhibitor | [CAS]
1832646-52-2 | [Synonyms]
GLS1 Inhibitor,GLS-1 Inhibitor
4-thiadiazol-2-yl]-benzeneacetamide
αS-methoxy-N-[5-[[(3R)-1-(3-pyridazinyl)-3-pyrrolidinyl]amino]-1
ΑS-METHOXY-N-[5-[[(3R)-1-(3-PYRIDAZINYL)-3-PYRROLIDINYL]AMINO]-1;3;4-THIADIAZOL-2-YL]-BENZENEACETAMIDE
Benzeneacetamide, α-methoxy-N-[5-[[(3R)-1-(3-pyridazinyl)-3-pyrrolidinyl]amino]-1,3,4-thiadiazol-2-yl]-, (αS)- | [Molecular Formula]
C19H21N7O2S | [MOL File]
1832646-52-2.mol | [Molecular Weight]
411.48 |
| Chemical Properties | Back Directory | [density ]
1.425±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml | [form ]
A crystalline solid | [pka]
7.42±0.50(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Description]
GLS1 inhibitor is an inhibitor of glutaminase 1 (GLS1; IC50 = 0.021 μM). It inhibits the growth of NCI H1703 non-small cell lung cancer (NSCLC) cells in vitro (GI50 = 0.011 μM). GLS1 inhibitor (100 mg/kg) reduces tumor growth, increases tumor levels of glutamine, and decreases tumor levels of glutamate and aspartate in an NCI H1703 mouse xenograft model. | [Uses]
GLS1 Inhibitor-1 (Compound 27) is an orally active inhibitor for glutaminase 1 (GLS1) with an IC50 of 0.021 μM. GLS1 Inhibitor-1 inhibits the proliferation of PC-3 with an IC50 of 0.3 nM. GLS1 Inhibitor-1 exhibits antitumor efficacy against NCI-H1703 with GI50 of 0.011 μM. GLS1 Inhibitor-1 exhibits moderate pharmacokinetic characteristics[1]. | [References]
[1] Finlay MRV, et al., Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models. J Med Chem. 2019 Jul 25;62(14):6540-6560. DOI:10.1021/acs.jmedchem.9b00260 |
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