Description
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.
Product information
CAS Number: 1799753-84-6
Molecular Weight: 496.42
Formula: C24H16F4N6O2
Synonym:
BAY 876
BAY-876
BAY876
Chemical Name: N4-[1-[(4-Cyanophenyl)methyl]-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-7-fluoro-2,4-Quinolinedicarboxamide
Smiles: CC1=C(NC(=O)C2=CC(=NC3=CC(F)=CC=C32)C(N)=O)C(=NN1CC1C=CC(=CC=1)C#N)C(F)(F)F
InChiKey: BKLJDIJJOOQUFG-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
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.
In Vivo:
BAY-876 (oral administration; 1.5-4.5 mg/kg/day for 28 days) causes a clear dose-dependent inhibition of tumorigenicity in mice.
References:
- 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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