CB-839

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CB-839 (Telalenastat) 是一种有效的、选择性的、口服生物可利用的谷氨酰胺酶抑制剂，对肾脏和大脑（GAC 和 KGA）中谷氨酰胺酶的 IC50 分别为 28 和 23 nM。

CB-839 (Telaglenastat) is a potent, selective, and orally bioavailable inhibitor of glutaminase with IC50 of 28 and 23 nM for glutaminase in kidney and brain (GAC and KGA), but not the liver form of glutaminase (GLS2, IC50>1 uM); demonstrates antiproliferative activity in triple-negative breast cancer (TNBC) cell line HCC-1806 and MDA-MB-231 with IC50 of 20-55 nM, decreases glutamine consumption, glutamate production, oxygen consumption, and the steady-state levels of glutathione and several tricarboxylic acid cycle intermediates; exhibits vivo efficacy in breast cancer xenograft models, both as a single agent and in combination with paclitaxel. Kidney Cancer Phase 2 Clinical(In Vitro):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.(In Vivo):Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC.

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. Cell Proliferation Assay Cell Line:HCC1806, MDA-MB-231 cells Concentration:0.1, 1, 10, 100, 1000 nM Incubation Time:72 hours Result:Has a potent effect on the proliferation of the two TNBC cell lines (IC50 of 49 nM and 26 nM for HCC1806 and MDA-MB-231 cells).Apoptosis AnalysisCell Line:MDA-MB-231, HCC1806 cells Concentration:1 μM Incubation Time:72 hours Result:Caspase 3/7 activation.

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.

CB839 | CB 839 | Telaglenastat

Others

Other Targets

GLUT

Cancer

Kidney Cancer

1439399-58-2

571.5741

C26H24F3N7O3S

>98% (HPLC)

DMSO: ≥ 30 mg/mL

O=C(NC1=CC=C(CCCCC2=NN=C(NC(CC3=NC=CC=C3)=O)S2)N=N1)CC4=CC(OC(F)(F)F)=CC=C4

2-Pyridineacetamide, N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-

(-20℃)

With Ice Pack

≥ 2 years