[CAS NO. 1439399-58-2] Telaglenastat (CB-839)
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PRODUCTS SPECIFICATIONS [1439399-58-2]
Store
Catalog
SLK-S7655
Brand
Selleck
CAS
1439399-58-2
DESCRIPTION [1439399-58-2]
Overview
| MDL | MFCD28167826 |
|---|---|
| Molecular Weight | 571.57 |
| Molecular Formula | C26H24F3N7O3S |
| SMILES | O=C(NC1=NN=C(CCCCC2=NN=C(NC(CC3=CC=CC(OC(F)(F)F)=C3)=O)C=C2)S1)CC4=NC=CC=C4 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7496 mL | 8.7478 mL | 17.4957 mL |
| 5 mM | 0.3499 mL | 1.7496 mL | 3.4991 mL |
| 10 mM | 0.1750 mL | 0.8748 mL | 1.7496 mL |
| 50 mM | 0.0350 mL | 0.1750 mL | 0.3499 mL |
Description
Telaglenastat (CB-839) is a potent, selective, and orally bioavailable inhibitor with of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces 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.
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%.
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