CB-839
Description In vitro In vivo- Product Name
- 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
- Formula Weight
- 571.57
- MOL File
- 1439399-58-2.mol
CB-839 Property
- 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.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 5.33717
- Product name
- GLS1 Inhibitor III, CB-839 - CAS 1439399-58-2 - Calbiochem
- Packaging
- 10mg
- Price
- $258
- Updated
- 2024/03/01
- Product number
- 22038
- Product name
- CB-839
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 22038
- Product name
- CB-839
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $302
- Updated
- 2024/03/01
- Product number
- 22038
- Product name
- CB-839
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $30
- Updated
- 2021/12/16
- Product number
- 22038
- Product name
- CB-839
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $95
- Updated
- 2024/03/01
CB-839 Chemical Properties,Usage,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
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View Lastest Price from CB-839 manufacturers
- Product
- CB-839 1439399-58-2
- Price
- US $0.00-0.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 1Ton
- Release date
- 2022-10-13