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CB-839

Cat. No. M3003
CB-839 Structure
Size Price Availability Quantity
5mg USD 105 In stock
10mg USD 180 In stock
50mg USD 510 In stock
100mg USD 740 In stock
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Quality Control
Biological Activity

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%.

Protocol
Cell Experiment
Cell lines HCC1806, MDA-MB-231, and T47D cells
Preparation method For viability assays, all cell lines are treated with CB-839 at the indicated concentrations for 72 hours and analyzed for antiproliferative effects using Cell Titer Glo.
Concentrations 1 mM
Incubation time 72 h
Animal Experiment
Animal models Female Scid/Bg mice bearing TNBC or JIMT-1 xenograft
Formulation 25% (w/v) hydroxypropyl-b-cyclodextrin (HPBCD) in 10 mmol/L citrate, pH 2
Dosages 200 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 571.57
Formula C26H24F3N7O3S
CAS Number 1439399-58-2
Purity 98.55%
Solubility 80 mg/mL warmed in DMSO
Storage at -20°C
References

Targeting glutaminolysis has antileukemic activity in acute myeloid leukemia and synergizes with BCL-2 inhibition.
Jacque N, et al. Blood. 2015 Sep 10;126(11):1346-56. PMID: 26186940.

Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer.
Gross MI, et al. Mol Cancer Ther. 2014 Apr;13(4):890-901. PMID: 24523301.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CB-839 supplier, GluR, inhibitors

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