CB-839

SKU: orb1226277

Description

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.

Key Properties

• CAS Number: 1439399-58-2
• MW: 571.5741
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₄F₃N₇O₃S
• SMILES: 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
• Target: GLUT
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• In Vivo:
  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.
• 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. 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 Analysis Cell line: MDA-MB-231, HCC1806 cells. Concentration: 1 μM. Incubation time: 72 hours. Result: Caspase 3/7 activation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CB839 | CB 839 | Telaglenastat

Quick Database Links

Gene Symbol

GLUT