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. |