[CAS NO. 1227158-85-1] BAY 87-2243

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PRODUCTS SPECIFICATIONS [1227158-85-1]

Catelog

SLK-S7309

Brand

Selleck

CAS

1227158-85-1

DESCRIPTION [1227158-85-1]

Overview

MDL	-
Molecular Weight	525.53
Molecular Formula	C26H26F3N7O2
SMILES	C(N1N=C(C2=NC(=NO2)C3=CC=C(OC(F)(F)F)C=C3)C=C1C)C=4C=C(N=CC4)N5CCN(CC5)C6CC6

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.9028 mL	9.5142 mL	19.0284 mL
5 mM	0.3806 mL	1.9028 mL	3.8057 mL
10 mM	0.1903 mL	0.9514 mL	1.9028 mL
50 mM	0.0381 mL	0.1903 mL	0.3806 mL

Description

BAY 87-2243 is a potent and selective inhibitor. BAY 87-2243 inhibits activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and . BAY 87-2243 exerts antitumor activity. Phase 1.

Targets

HIF-1 ^[1]
(Cell-free assay)

In vitro

BAY 87-2243 inhibits HIF-1 reporter gene activity and CA9 protein expression with IC50 of 0.7 nM and 2 nM, respectively. In hypoxic lung cancer H460 cells, BAY 87-2243 suppresses HIF target gene expression, and inhibits HIF-1α protein accumulation. Under glucose depletion, BAY 87-2243 inhibits cell proliferation via interference with mitochondrial function.

In vivo

In H460 xenograft mouse model, BAY 87-2243 (4 mg/kg p.o.) reduces tumor weight, HIF-1α protein, and HIF-1 target gene expression levels.

References

[1] Ellinghaus P, et al. Cancer Med. 2013, 2(5), 611-624.

Synonyms

Piperazine, 1-cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]-

1-Cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]piperazine

BAY 87-2243