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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-1 (GLS1) in kidney and brain (GAC and KGA), but not the liver form of glutaminase (GLS2, IC50>1 uM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $78 | In stock | |
| 10 mg | $118 | In stock | |
| 50 mg | $258 | In stock | |
| 100 mg | $398 | In stock | |
| 250 mg | 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-1 (GLS1) 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 | 571.57 | |
| Formula | C26H24F3N7O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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. Chakrabarti G, et al. Cancer Metab. 2015 Oct 12;3:12.
3. Jacque N, et al. Blood. 2015 Sep 10;126(11):1346-56.
4. Zimmermann SC, et al. ACS Med Chem Lett. 2016 Mar 13;7(5):520-4.
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