CB-839 | Glutaminase inhibitor

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 from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Shipping Code:
RT

Available Options

Size :PriceQuantity 
5 mg$55.00
25 mg$175.00
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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

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 from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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