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Chemical Structure : CB-839
CAS No.: 1439399-58-2
Catalog No.: PC-42933Not For Human Use, Lab Use Only.
CB-839 (Telaglenastat) is a potent, selective, and orally bioavailable inhibitor of glutaminase with IC50 of 28 and 23 nM for glutaminase in kidney and brain (GAC and KGA), but not the liver form of glutaminase (GLS2, IC50>1 uM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $228 | In stock | |
| 50 mg | $378 | In stock | |
| 100 mg | $588 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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CB-839 (Telaglenastat) is a potent, selective, and orally bioavailable inhibitor of glutaminase with IC50 of 28 and 23 nM for glutaminase in kidney and brain (GAC and KGA), but not the liver form of glutaminase (GLS2, IC50>1 uM).
CB-839 (Telaglenastat) demonstrates antiproliferative activity in triple-negative breast cancer (TNBC) cell line HCC-1806 and MDA-MB-231 with IC50 of 20-55 nM.
CB-839 (Telaglenastat) decreases glutamine consumption, glutamate production, oxygen consumption, and the steady-state levels of glutathione and several tricarboxylic acid cycle intermediates.
CB-839 (Telaglenastat) exhibits vivo efficacy in breast cancer xenograft models, both as a single agent and in combination with paclitaxel.
| M.Wt | 571.5741 | |
| Formula | C26H24F3N7O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 30 mg/mL |
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| Chemical Name/SMILES |
2-Pyridineacetamide, N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]- |
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1. Gross MI, et al. Mol Cancer Ther. 2014 Apr;13(4):890-901.
2. Jacque N, et al. Blood. 2015 Sep 10;126(11):1346-56.
3. Chakrabarti G, et al. Cancer Metab. 2015 Oct 12;3:12.
4. Zimmermann SC, et al. ACS Med Chem Lett. 2016 Mar 13;7(5):520-4.
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