产品
编 号：F762870
分子式：C37H52N6O3S
分子量：660.91
分子式：C37H52N6O3S
分子量：660.91
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CAS No: 3033615-55-0
产品详情
生物活性：
GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis.
体内研究：
GLS1 Inhibitor-6 (oral gavage; 100 mg/kg; once daily; 28 d) treatment inhibits tumor growth in the preclinical mouse models.Animal Model:Rats
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). ParametersI.V.P.O.
t1/2 (h)9.919.8
CL (L/h/kg)6.133.4
Cmax ng/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
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.
体外研究：
GLS1 Inhibitor-6 (0-10 μM) inhibts cancer cell growth.GLS1 Inhibitor-6 (1-10 μM, 48 h) can induce A549 cell apoptosis.GLS1 Inhibitor-6 (50-800 nM, 48 h) can induce cell cycle arrest in the G1 phase.
GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis.
体内研究：
GLS1 Inhibitor-6 (oral gavage; 100 mg/kg; once daily; 28 d) treatment inhibits tumor growth in the preclinical mouse models.Animal Model:Rats
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). ParametersI.V.P.O.
t1/2 (h)9.919.8
CL (L/h/kg)6.133.4
Cmax ng/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
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.
体外研究：
GLS1 Inhibitor-6 (0-10 μM) inhibts cancer cell growth.GLS1 Inhibitor-6 (1-10 μM, 48 h) can induce A549 cell apoptosis.GLS1 Inhibitor-6 (50-800 nM, 48 h) can induce cell cycle arrest in the G1 phase.
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