CB-839

SKU: orb1300456

Description

Telaglenastat (CB-839) is an orally bioavailable, selective, and reversible inhibitor of glutaminase 1 (GLS1). It exhibits antitumor activity by disrupting cancer cell metabolism and inducing autophagy, as demonstrated in both in vitro and in vivo cancer research models.

Research Area

Cell Biology, Neuroscience

Key Properties

• CAS Number: 1439399-58-2
• MW: 571.6
• Purity: >98%
• Formula: C₂₆H₂₄F₃N₇O₃S
• SMILES: FC(F)(F)Oc1cccc(CC(=O)Nc2ccc(CCCCc3nnc(NC(=O)Cc4ccccn4)s3)nn2)c1
• Target: Glutaminase
• Solubility: Soluble in DMSO (20 mg/ml)

Bioactivity

• Target IC50:
  CT-26 cells:0.42 μM|MDA-MB-436 cells:0.52 μM|TNBC:20-55 nM|HCC827 cells:51.42 μM|endogenous glutaminase (mouse kidney):23 nM|HCC1806 cells:100 nM|H22 cells:> 10 μM|NCI-H4 cells:0.036 μM|HT1080 cells:44.38 μM|CAKI-1 cells:0.04 μM|NCI-H358 cells:> 1 μM|endogenous glutaminase (mouse brain):28 nM|A549 cells:0.026 μM|Glutaminase:24 nM|HCT116 cells:0.028 μM
• In Vivo:
  In the mouse TNBC model, single agent CB-839 (200 mg/kg, p.o.) suppresses tumor growth by 61% relative to vehicle control. In the mouse JIMT-1 xenograft model, CB-839 alone (200 mg/kg, p.o.) results in 54% tumor growth inhibition (TGI) relative to vehicle control, combination of CB-839 (200 mg/kg, p.o.) with paclitaxel (10 mg/kg, p.o.) largely suppresses the regrowth of the tumors resulting in a TGI relative to vehicle control of 100%.
• In Vitro:
  CB-839 exhibits time-dependent and slowly reversible kinetics. IC50 values for glutaminase inhibition by CB-839 following preincubation with rHu-GAC for-1 hour are < 50 nmol/L, at least 13-fold lower than with BPTES. CB-839 has antiproliferative activity in a triple-negative breast cancer (TNBC) cell line, HCC-1806, while no antiproliferative activity is observed in an estrogen receptor–positive cell line, T47D.
• Cell Research:
  For viability assays, all cell lines are treated with CB-839 at the indicated concentrations for 72 hours and analyzed for antiproliferative effects using Cell Titer Glo.(Only for Reference)

Storage & Handling

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

Alternative Names

Telaglenastat

Compound Identifiers

PubChem CID

71577426