BAY 87-2243 --- Hypoxia-inducible Factor-1 (HIF-1) Inhibitor

BAY 87-2243 is a highly potent and selective inhibitor of hypoxia-induced gene activation, which has antitumor activities by inhibition of mitochondrial complex I. BAY 87-2243 mproves local tumor control after fractionated irradiation in a schedule-dependent manner in head and neck human xenografts. BAY-87-2243 markedly decreased nuclear HIF-1α expression and pimonidazole hypoxic fraction already after 3 days of drug treatment. BAY-87-2243 prior to RT significantly reduced TCD50 from 123 to 100 Gy (p=0.037). Additional BAY-87-2243 application during RT did not decrease TCD50.

Product information

CAS Number: 1227158-85-1

Molecular Weight: 525.53

Formula: C26H26F3N7O2

Chemical Name: 5-(1-((2-(4-cyclopropylpiperazin-1-yl)pyridin-4-yl)methyl)-5-methyl-1H-pyrazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole

Smiles: CC1=CC(=NN1CC1C=C(N=CC=1)N1CCN(CC1)C1CC1)C1=NC(=NO1)C1C=CC(=CC=1)OC(F)(F)F

InChiKey: CDJNNOJINJAXPV-UHFFFAOYSA-N

InChi: InChI=1S/C26H26F3N7O2/c1-17-14-22(25-31-24(33-38-25)19-2-6-21(7-3-19)37-26(27,28)29)32-36(17)16-18-8-9-30-23(15-18)35-12-10-34(11-13-35)20-4-5-20/h2-3,6-9,14-15,20H,4-5,10-13,16H2,1H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 1 mM; EtOH up to 15 mM (heating)

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: ≥12 months 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 87-2243 was used at 0.1-10 µM final concentration in various in vitro assays.

In Vivo:

BAY 87-2243 was dosed to Mice bearing lung carcinoma H460 xenografts via oral gavage at 4 mg/kg once per day. Formulation is 1% (v/v) solution of ethanol/solutol/water (10/40/50%).

References:

1. Ellinghaus P, et al. BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. (2013) Cancer Med. 2(5):611-24.

Products are for research use only. Not for human use.

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