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Background Information:
CB-839 (Telaglenastat) is a clinical-stage, orally bioavailable inhibitor of the glutaminase 1 (GLS1) splice variants, kidney-type (KGA) and glutaminase C (GAC). It inhibits human recombinant GAC (IC50 < 50 nM), and GLS1 activity in tissue homogenates (IC50s = 28 and 23 nM, respectively for brain and kidney), but not GLS2 (IC50 > 1,000 nM from liver). Displays antiproliferative activity against the triple-negative breast cancer (TNBC) cell lines HCC1806 and MDA-MB-231 (IC50s = 49 and 26 nM, respectively) but not against estrogen receptor-positive T47D cells (IC50 > 1,000 nM). In a patient-derived TNBC mouse xenograft model, CB-839 (200 mg/kg, p.o.) inhibits tumor growth by 61% relative to vehicle control. It also possesses antiproliferative properties in vitro against acute myeloid leukemia (AML) and in synergy with erlotinib (Prod No. CT-EL002) in EGFR-driven non-small cell lung cancer (NSCLC) in vitro and in xenografts (ref 1, 2, 3).
APIM050347: CB-839 (TELAGLENASTAT)
CAS No.: 1439399-58-2.
Molecular Formula: C26H24F3N7O3S.
Molecular Weight: 571.6.
Purity: 99.9% by HPLC.
QC: HPLC, 1H-NMR and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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