Home Cart Sign in  
Chemical Structure| 1439399-58-2 Chemical Structure| 1439399-58-2

Structure of Telaglenastat
CAS No.: 1439399-58-2

Chemical Structure| 1439399-58-2

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

Telaglenastat (CB-839) is a first-in-class, selective, reversible, and orally active glutaminase 1 (GLS1) inhibitor. It selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) with IC50 values of 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat induces autophagy and has antitumor activity.

Synonyms: CB-839; GLS1 Inhibitor III

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of Telaglenastat

CAS No. :1439399-58-2
Formula : C26H24F3N7O3S
M.W : 571.57
SMILES Code : 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
Synonyms :
CB-839; GLS1 Inhibitor III
MDL No. :MFCD28167826
InChI Key :PRAAPINBUWJLGA-UHFFFAOYSA-N
Pubchem ID :71577426

Safety of Telaglenastat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • glutaminase

    Glutaminase, IC50:24 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
FaDu cells 10 nM 48 h Telaglenastat did not significantly affect the size of FaDu spheroids. Cancer Lett. 2021 Apr 1;502:180-188.
Pmel-1 T cells 1 µM 6 h CB-839 minimally altered glutamate and αKGA levels in Pmel-1 T cells Mol Cancer Ther. 2021 Mar;20(3):500-511.
SK-LMS-1 cells 1 μM 48 h To evaluate the effect of CB-839 on the proliferation and viability of SK-LMS-1 cells, results showed that CB-839 significantly inhibited cell proliferation and viability. Nat Commun. 2020 Jan 24;11(1):498.
HT1080 cells 1 μM 48 h To evaluate the effect of CB-839 on the proliferation and viability of HT1080 cells, results showed that CB-839 significantly inhibited cell proliferation and viability. Nat Commun. 2020 Jan 24;11(1):498.
KPH2-7215 cells 1 μM 48 h To evaluate the effect of CB-839 on the proliferation and viability of KPH2-7215 cells, results showed that CB-839 significantly inhibited cell proliferation and viability. Nat Commun. 2020 Jan 24;11(1):498.
KP-6634 cells 1 μM 48 h To evaluate the effect of CB-839 on the proliferation and viability of KP-6634 cells, results showed that CB-839 significantly inhibited cell proliferation and viability. Nat Commun. 2020 Jan 24;11(1):498.
HN5 cells 10 nM 48 h Telaglenastat significantly reduced the size of CAL-27 and HN5 spheroids and increased oxidative stress and DNA damage. Cancer Lett. 2021 Apr 1;502:180-188.
CAL-27 cells 10 nM 48 h Telaglenastat significantly reduced the size of CAL-27 and HN5 spheroids and increased oxidative stress and DNA damage. Cancer Lett. 2021 Apr 1;502:180-188.
Patient MCL cells 11.3 µM 72 h Telaglenastat inhibited the proliferation of patient MCL cells with an IC50 of 11.3 µM. Haematologica. 2023 Jun 1;108(6):1616-1627.
MCL cell lines 0.22-9.2 µM 72 h Telaglenastat inhibited the proliferation of MCL cell lines with an IC50 of 0.22-9.2 µM. Haematologica. 2023 Jun 1;108(6):1616-1627.
A375HG melanoma cells 1 µM 6 h CB-839 significantly reduced glutamate and αKGA levels in A375HG cells Mol Cancer Ther. 2021 Mar;20(3):500-511.
autologous tumor-infiltrating lymphocytes (TILs) 1 µM 12 h CB-839 caused minimal inhibition of glutamine consumption and OCR in TILs Mol Cancer Ther. 2021 Mar;20(3):500-511.
patient-derived melanoma cell lines 1 µM 12 h CB-839 significantly reduced glutamine consumption in melanoma cells Mol Cancer Ther. 2021 Mar;20(3):500-511.
SiHa PTEN−/− cells 200 nM 96 h Assess cell viability, Telaglenastat treatment significantly reduced cell survival Mol Cancer Ther. 2020 Dec;19(12):2465-2475.
SiHa cells 200 nM 96 h Assess cell viability, Telaglenastat treatment had minimal effect on cell survival Mol Cancer Ther. 2020 Dec;19(12):2465-2475.
CaSki cells 200 nM 96 h Assess cell viability, Telaglenastat treatment reduced cell survival Mol Cancer Ther. 2020 Dec;19(12):2465-2475.
LN229 20 nM 24 h Evaluate the cytotoxicity of nanomedicine on LN229 cells, results showed weaker inhibition of cell growth at 20 nM concentration Int J Mol Sci. 2022 May 13;23(10):5479.
U87 20 nM 24 h Evaluate the cytotoxicity of nanomedicine on U87 cells, results showed significant inhibition of cell growth at 20 nM concentration Int J Mol Sci. 2022 May 13;23(10):5479.
NCH644 20 nM 24 h Evaluate the cytotoxicity of nanomedicine on NCH644 cells, results showed significant inhibition of cell growth at 20 nM concentration Int J Mol Sci. 2022 May 13;23(10):5479.
GBM1 20 nM 24 h Evaluate the cytotoxicity of nanomedicine on GBM1 cells, results showed significant inhibition of cell growth at 20 nM concentration Int J Mol Sci. 2022 May 13;23(10):5479.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice KP and KPH2 mouse models Oral 200 mg/kg Twice daily for 2-3 weeks To evaluate the effect of CB-839 on tumour growth in KP and KPH2 mouse models, results showed that CB-839 significantly inhibited tumour growth. Nat Commun. 2020 Jan 24;11(1):498.
Nude mice HN5 and CAL-27 xenograft models Oral gavage 200 mg/kg Twice daily for 14 days Combination treatment of telaglenastat with ionizing radiation significantly reduced tumor volume in CAL-27 xenograft models compared to telaglenastat or ionizing radiation alone. Cancer Lett. 2021 Apr 1;502:180-188.
NSG mice Z138 cell-derived xenograft model Oral 200 mg/kg Twice daily, continuous treatment Telaglenastat significantly inhibited the growth of Z138 xenograft tumors and prolonged mouse survival. Haematologica. 2023 Jun 1;108(6):1616-1627.
Mice B16-F10 melanoma model Oral 200 mg/kg Twice daily for one month CB-839 in combination with Pmel-1 T cell therapy significantly enhanced anti-tumor activity Mol Cancer Ther. 2021 Mar;20(3):500-511.
Nude mice CaSki and SiHa xenograft models Oral gavage 50 mg/kg, 100 mg/kg, 200 mg/kg Three times per week for 37 days Assess the effect of Telaglenastat monotherapy on tumor growth, Telaglenastat significantly inhibited tumor growth Mol Cancer Ther. 2020 Dec;19(12):2465-2475.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.75mL

0.35mL

0.17mL

8.75mL

1.75mL

0.87mL

17.50mL

3.50mL

1.75mL

References

 

Historical Records

Categories