GLS1 Inhibitor-6 (Compound 24y) 是一种具有口服活性的、强效和选择性的谷氨酰胺酶 1 (GLS1) 抑制剂 (IC50=68 nM)，对 GLS2 显示出 220 倍的选择性。GLS1 Inhibitor-6 可诱导凋亡，并表现出良好的抗肿瘤活性和抗癌细胞增殖活性。
| 生物活性 | GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selectiveglutaminase1(GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and inducesapoptosis[1]. |
| IC50& Target | |
体外研究
(In Vitro) | GLS1 Inhibitor-6 (0-10 μM) inhibts cancer cell growth[1].
GLS1 Inhibitor-6 (1-10 μM, 48 h) can induce A549 cell apoptosis[1].
GLS1 Inhibitor-6 (50-800 nM, 48 h) can induce cell cycle arrest in the G1 phase[1].
Cell Viability Assay[1] | Cell Line: | A549 and HCT116 cell | | Concentration: | 0-10 μM | | Incubation Time: | | | Result: | Inhibited A549 and HCT116 cell growth with IC50s of 0.57 and 0.42 μM, respectively. |
Apoptosis Analysis[1] | Cell Line: | A549 cell | | Concentration: | 1, 5, and 10 μM | | Incubation Time: | 48 h | | Result: | Showed the population of apoptotic cells to 84% at the concentration of 10 μM. |
Cell Cycle Analysis[1] | Cell Line: | A549 cell | | Concentration: | 50, 100, 200, 400 and 800 nM | | Incubation Time: | 48 h | | Result: | Resulted in G1 phase cell cycle arrest in a dose-dependent manner, and decreased proportion of cells in the S phase. |
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体内研究
(In Vivo) | GLS1 Inhibitor-6 (oral gavage; 100 mg/kg; once daily; 28 d) treatment inhibits tumor growth in the preclinical mouse models[1].
| Animal Model: | Rats[1] | | Dosage: | 3 mg/kg | | Administration: | I.V. and P.O.; 3 mg/kg; once | | Result: | 1.19The pharmacokinetic parameters of GLS1 Inhibitor-5 (compound 24y)[1].
| Parameters | I.V. | P.O. | | t1/2(h) | 9.9 | 19.8 | | CL (L/h/kg) | 6.1 | 33.4 | | Cmaxng/mL | 699.1 | 41.3 | | AUC0–t(ng·h/mL) | 2092.3 | 251.6 | | F% | 12.4 | | |
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| Animal Model: | Human non-small cell lung A549 xenograft tumor model, GLS1 high-expression HCT116 xenograft tumor model[1] | | Dosage: | 100 mg/kg | | Administration: | Oral gavage; 100 mg/kg; once daily; 28 days | | Result: | Showed 40.9% tumor growth inhibition in A549 model, and showed 42% tumor growth inhibition in HCT116 model. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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