Structure of Telaglenastat
CAS No.: 1439399-58-2
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
|
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. | PMC7897292 |
Pmel-1 T cells | 1 µM | 6 h | CB-839 minimally altered glutamate and αKGA levels in Pmel-1 T cells | PMC7933078 |
A375HG melanoma cells | 1 µM | 6 h | CB-839 significantly reduced glutamate and αKGA levels in A375HG cells | PMC7933078 |
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. | PMC6981153 |
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. | PMC6981153 |
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. | PMC6981153 |
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. | PMC6981153 |
HN5 cells | 10 nM | 48 h | Telaglenastat significantly reduced the size of CAL-27 and HN5 spheroids and increased oxidative stress and DNA damage. | PMC7897292 |
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. | PMC7897292 |
Patient MCL cells | 11.3 µM | 72 h | Telaglenastat inhibited the proliferation of patient MCL cells with an IC50 of 11.3 µM. | PMC10230437 |
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. | PMC10230437 |
Autologous tumor-infiltrating lymphocytes (TILs) | 1 µM | 12 h | CB-839 caused minimal inhibition of glutamine consumption and OCR in TILs | PMC7933078 |
Patient-derived melanoma cell lines | 1 µM | 12 h | CB-839 significantly reduced glutamine consumption in melanoma cells | PMC7933078 |
SiHa PTEN−/− cells | 200 nM | 96 h | Assess cell viability, Telaglenastat treatment significantly reduced cell survival | PMC8208465 |
SiHa cells | 200 nM | 96 h | Assess cell viability, Telaglenastat treatment had minimal effect on cell survival | PMC8208465 |
CaSki cells | 200 nM | 96 h | Assess cell viability, Telaglenastat treatment reduced cell survival | PMC8208465 |
LN229 | 20 nM | 24 h | Evaluate the cytotoxicity of nanomedicine on LN229 cells, results showed weaker inhibition of cell growth at 20 nM concentration | PMC9141725 |
U87 | 20 nM | 24 h | Evaluate the cytotoxicity of nanomedicine on U87 cells, results showed significant inhibition of cell growth at 20 nM concentration | PMC9141725 |
NCH644 | 20 nM | 24 h | Evaluate the cytotoxicity of nanomedicine on NCH644 cells, results showed significant inhibition of cell growth at 20 nM concentration | PMC9141725 |
GBM1 | 20 nM | 24 h | Evaluate the cytotoxicity of nanomedicine on GBM1 cells, results showed significant inhibition of cell growth at 20 nM concentration | PMC9141725 |
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. | PMC6981153 |
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. | PMC7897292 |
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. | PMC10230437 |
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 | PMC7933078 |
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 | PMC8208465 |
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 |
Tags: Telaglenastat | CB-839 | CB839 | CB 839 | Glutaminase | Autophagy | selective | triple-negative | breast | cancer | TNBC | antiproliferative| PDAC | cell | splice | variants | glutamine metabolism | glutamine-addicted cancer | metabolic stress | glutaminase inhibitor | cancer metabolism | glutamine addiction | 1439399-58-2
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