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Home > Products >  Telaglenastat (CB-839)

Telaglenastat (CB-839) CAS NO.1439399-58-2

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Keywords

  • Telaglenastat
  • CB-839
  • 1439399-58-2

Quick Details

  • ProName: Telaglenastat (CB-839)
  • CasNo: 1439399-58-2
  • Molecular Formula: C26H24F3N7O3S
  • ProductionCapacity: Metric Ton/Day
  • Purity: >97%
  • LimitNum: 0 Metric Ton

Superiority

Biological Activity

Description Telaglenastat (CB-839) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1.
Targets
Glutaminase [1]
(Cell-free assay)
24 nM
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.[1]
Cell Data
 
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 cells Cytotoxicity assay   6 days   Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry, IC50=0.033 μM 26988803
TNBC cell lines Growth inhibiton assay 1 μM 4 days   CB-839 treatment induced cell loss or decreased cell proliferation by more than 50% in six cell lines (HCC1806, HCC1143, HCC38, MDA-MB-436, MDA-MB-231 and Hs578T); the other six cell lines (HCC1937, HCC70, BT549, MDA-MB-157, MDA-MB-453 and MDA-MB468) were either not affected or had their cell proliferation affected by less than 50% and were called resistant. 31040181
MM.1S BzR cells Function assay 5 μM 16 hours   treatment with CB-839 significantly repressed oxygen consumption rate in proteasome-inhibitor resistant cells. 28415782

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot 29019707
Growth inhibition assay 28967864
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%.[1]

 

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