CB-839

CB-839

Catalog Number:
L002370659APE
Mfr. No.:
APE-B4799
Price:
$255
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      • Overview
        • Please contact us at for specific academic pricing.

          Background

          CB-839(Telaglenastat) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC(glutaminase C)[1].
          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[1].
          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%[1].

          [1]. Gross MI, et al. Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014 Apr;13(4):890-901.

      • Properties
        • Alternative Name
          2-(pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide
          CAS Number
          1439399-58-2
          Molecular Formula
          C26H24F3N7O3S
          Molecular Weight
          571.57
          Purity
          98.00%
          Solubility
          ≥28.6 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Momcilovic M, Bailey ST, et al. "The GSK3 Signaling Axis Regulates Adaptive Glutamine Metabolism in Lung Squamous Cell Carcinoma." Cancer Cell. 2018 May 14;33(5):905-921.e5. PMID:29763624

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