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编 号：F747661
分子式：C26H25ClF3N7O3S
分子量：608.04
分子式：C26H25ClF3N7O3S
分子量：608.04
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CAS No: 1874231-60-3
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生物活性：
Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity.
体内研究：
Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC.Animal Model:Female nu/nu mice with age 4–6 weeks (TNBC patient-derived xenograft model)
Dosage:200 mg/kg
Administration:Oral administration; twice daily for 28 days
Result:Suppressed tumor growth by 61% relative to vehicle control at the end of study.
体外研究：
Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC50s of 49 nM and 26 nM, respectively.Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells.
Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity.
体内研究：
Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC.Animal Model:Female nu/nu mice with age 4–6 weeks (TNBC patient-derived xenograft model)
Dosage:200 mg/kg
Administration:Oral administration; twice daily for 28 days
Result:Suppressed tumor growth by 61% relative to vehicle control at the end of study.
体外研究：
Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC50s of 49 nM and 26 nM, respectively.Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells.
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