CB-839
- CAS No.
- 1439399-58-2
- Chemical Name:
- CB-839
- Synonyms
- CB-839;CPD1593;CS-1813;Telaglenastat;CB-839,TELAGLENASTAT;CB839 ;CB 839 ;CB-839;Telaglenastat (CB-839);GLS1 Inhibitor III, CB-839 - CAS 1439399-58-2 - Calbiochem;N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-2-pyridineacetamide;2-Pyridineacetamide, N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-
- CBNumber:
- CB92718863
- Molecular Formula:
- C26H24F3N7O3S
- Molecular Weight:
- 571.57
- MDL Number:
- MFCD28167826
- MOL File:
- 1439399-58-2.mol
| Melting point | 186- 189° C |
|---|---|
| Density | 1.430±0.06 g/cm3(Predicted) |
| storage temp. | +2C to +8C |
| solubility | Soluble in DMSO. |
| form | Yellow solid |
| pka | 8.25±0.50(Predicted) |
| color | Pale yellow |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months. |
| FDA UNII | U6CL98GLP4 |
| NCI Drug Dictionary | telaglenastat |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
CB-839 price More Price(31)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 5.33717 | GLS1 Inhibitor III, CB-839 - CAS 1439399-58-2 - Calbiochem | 1439399-58-2 | 10mg | $258 | 2024-03-01 | Buy |
| Cayman Chemical | 22038 | CB-839 ≥98% | 1439399-58-2 | 5mg | $57 | 2024-03-01 | Buy |
| Cayman Chemical | 22038 | CB-839 ≥98% | 1439399-58-2 | 50mg | $302 | 2024-03-01 | Buy |
| Cayman Chemical | 22038 | CB-839 ≥98% | 1439399-58-2 | 1mg | $30 | 2021-12-16 | Buy |
| Cayman Chemical | 22038 | CB-839 ≥98% | 1439399-58-2 | 10mg | $95 | 2024-03-01 | Buy |
CB-839 Chemical Properties,Uses,Production
Description
CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. Phase 1.
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%.
Description
CB-839 (14393999-58-2)?is a potent (IC50?= 24 nM), selective and orally bioavailable inhibitor of glutaminase (KGA and GAC).1?CB-839 displayed an antiproliferative effect in the triple-negative breast cancer cell line, HCC-1806, but no activity in the estrogen receptor-positive cell line T47D.? CB-839 was able to cause proliferation arrest and apoptosis in acute myeloid leukemia cells without causing cytotoxicity against normal human CD34(+) progenitors.2? Aspartate-glutamate carrier 1 (AGC1) inhibition can synergize with CB-839 to limit tumor growth.3
Uses
CB-839 performs an antileukemic activity. It Inhibits GLS1 genes and reduces oxidative phosphorylation leading to leukamic cell proliferation arrest and apoptosis.
storage
Store at -20°C
References
1) Gross?et al. (2014),?Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer; Mol. Cancer Ther.,13?890 2) Jacque?et al. (2015),?Targeting glutaminolysis has antileukemic activity in acute myeloid leukemia and synergizes with BCL-2 inhibition; Blood,?126?1346 3) Alkan?et al.?(2018)?Cytosolic Aspartate Availability Determines Cell Survival When Glutamine is Limiting; Cell Metabolism?28?1
CB-839 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | fandachem@gmail.com | China | 9341 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| Changzhou PBpharmaceutical R&D Co.,Ltd | 0519-83990708 | info@pbpharm.com | CHINA | 498 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| Alfa Chemistry | +1-5166625404 | Info@alfa-chemistry.com | United States | 21317 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
| Henan Aochuang Chemical Co.,Ltd. | +86-0371-63689365 +8618638391208 | sales@aochuangchem.com | China | 9425 | 58 |
