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Product Details

CB-839 | Glutaminase inhibitor

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

References/Citations
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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Focus Biomolecules cell signaling reagent supplier, chemical structure of CB-839 | Glutaminase inhibitor | CAS 1439399-58-2

Catalog#  10-4556

$55.00
Quantity
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CAS:
1439399-58-2
Catalog Number:
10-4556
Activity:
Glutaminase inhibitor
Chemical Name:
2-(Pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide
Molecular Weight:
571.57
Molecular Formula:
C26H24F3N7O3S
Solubility:
Soluble in DMSO.
Physical Properties:
Pale yellow solid
Purity:
>97% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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