BAY-876 is a potent and Selective GLUT1 Inhibitor. BAY-876 showed good metabolic stability in vitro and high oral bioavailability in vivo. GLUT1 overexpression has been reported in many types of human cancers, including those of brain,6 breast, colon, kidney, lung, ovary, and prostate, and is correlated with advanced cancer stages and poor clinical outcomes.
Chemical Formula: C24H16F4N6O2
Exact Mass: 496.1271
Molecular Weight: 496.4256
Elemental Analysis: C, 58.07; H, 3.25; F, 15.31; N, 16.93; O, 6.45
Chemical Name: N4-[1-[(4-Cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoro-2,4-Quinolinedicarboxamide
InChi Code: InChI=1S/C24H16F4N6O2/c1-12-20(21(24(26,27)28)33-34(12)11-14-4-2-13(10-29)3-5-14)32-23(36)17-9-19(22(30)35)31-18-8-15(25)6-7-16(17)18/h2-9H,11H2,1H3,(H2,30,35)(H,32,36)
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
BAY-876 (25-75 nM; 24 and 72 hours) has the growth-inhibitory effect and leads to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells.
BAY-876 (oral administration; 1.5-4.5 mg/kg/day for 28 days) causes a clear dose-dependent inhibition of tumorigenicity in mice.
Siebeneicher H, Cleve A, Rehwinkel H, Neuhaus R, Heisler I, Müller T, Bauser M, Buchmann B. Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876. ChemMedChem. 2016 Oct 19;11(20):2261-2271. doi: 10.1002/cmdc.201600276. PubMed PMID: 27552707; PubMed Central PMCID: PMC5095872.
Products are for research use only. Not for human use.
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