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

Catalog No. size PriceQuantity
M60217-2S 2 mg solid $119
M60217-10S 10mg solid $482


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


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%).


  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.


Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed