Telaglenastat

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, Metabolism Research, Protein Biochemistry

Key Properties

• CAS Number: 1439399-58-2
• MW: 571.57
• Purity: >99.99% (May vary between batches)
• Formula: C₂₆H₂₄F₃N₇O₃S
• SMILES: FC(F)(F)Oc1cccc(CC(=O)Nc2ccc(CCCCc3nnc(NC(=O)Cc4ccccn4)s3)nn2)c1
• Target: Autophagy,transporter,Glutaminase
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:121.3 mg/mL (212.22 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:9.3 mg/mL (16.27 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

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: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, PDAC, Inhibitor, HCC-1806, Glutaminase, GLUT, Autophagy, antiproliferative, CB839, CB-839, CB 839, cancer, breast, cell, selective, TNBC, splice, Telaglenastat, triple-negative, variants

Compound Identifiers

PubChem CID

71577426