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GLS1 Inhibitor-6
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GLS1 Inhibitor-6图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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

IC50: 68 nM (GLS1)[1]

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.
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].
ParametersI.V.P.O.
t1/2(h)9.919.8
CL (L/h/kg)6.133.4
Cmaxng/mL699.141.3
AUC0–t(ng·h/mL)2092.3251.6
F%12.4
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.
分子量

660.91

Formula

C37H52N6O3S

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.