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BAY 87-2243HIF-1 inhibitor,potent and selective

BAY 87-2243

Catalog No. B1115
Size Price Stock Qty
10mM (in 1mL DMSO) $200.00 In stock
10mg $124.00 In stock
50mg $523.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

BAY 87-2243

Protocol

Cell experiment [1, 2]:

Cell lines

H460, RCC4 cells, BRAFWT melanoma cells, and BRAFV600E melanoma cells

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1, 10, 100, and 1000 nmol/L BAY 87-2243 for 16 h; or 10 nmol/L BAY 87-2243 for 24, 48, and 72 h

Applications

BAY 87-2243 (100 nmol/L) significantly inhibited the expression of HIF target gene, including ANGPTL4, ADM, and CA9 in hypoxic H460 cells. Moreover, BAY 87-2243 inhibited mitochondrial complex I and induced cell death of melanoma cells in a dose-dependent manner.

Animal experiment [1, 2]:

Animal models

H460 xenograft tumors model; melanoma xenografts (G-361 and SK-MEL-28); patient-derived (MEXF 276 and MEXF 1732) melanoma xenograft tumors model

Dosage form

0.5, 1.0, 2.0, and 4.0 mg/kg, oral administration, once daily, for 21 days; or 9 mg/kg, oral gavage (p.o.)., once a day

Applications

BAY 87-2243 dose-dependently decreased tumor weight, hypoxia-inducible factor (HIF)-1a protein, and HIF-1 target gene expression levels in H460 xenograft tumors. Moreover, BAY 87-2243 significantly reduced tumor growth in all BRAF mutant melanoma xenografts.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Ellinghaus, P., Heisler, I., Unterschemmann, K., Haerter, M., Beck, H., Greschat, S., Ehrmann, A., Summer, H., Flamme, I., Oehme, F., Thierauch, K., Michels, M., Hess-Stumpp, H. and Ziegelbauer, K. (2013) BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. Cancer Med. 2, 611-6242

2. Schockel, L., Glasauer, A., Basit, F., Bitschar, K., Truong, H., Erdmann, G., Algire, C., Hagebarth, A., Willems, P. H., Kopitz, C., Koopman, W. J. and Heroult, M. (2015) Targeting mitochondrial complex I using BAY 87-2243 reduces melanoma tumor growth. Cancer Metab. 3, 11

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Chemical Properties

Cas No. 1227158-85-1 SDF Download SDF
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
Canonical SMILES CC1=CC(C2=NC(C3=CC=C(OC(F)(F)F)C=C3)=NO2)=NN1CC4=CC=NC(N5CCN(C6CC6)CC5)=C4
Formula C26H26F3N7O2 M.Wt 525.53
Solubility >8.8mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

BAY 87-2243 is a selective inhibitor of HIF-1 induced gene activation [1].

In HCT-116 cells, BAY 87-2243 inhibits the hypoxia increased HRE-dependent luciferase expression with IC50 value of 0.7nM and inhibits the expression of HIF target gene CA9 with IC50 value of 2nM. In H460 cells cultured under hypoxia, BAY 87-2243 suppresses the expression of HIF-1 target genes including CA9, adrenomedullin and angiopoietin-like protein-4. BAY 87-2243 also inhibits both HIF-1α and HIF-2α protein accumulation in this cell line. Moreover, in mice model bearing H460 xenograft, treatment of BAY 87-2243 reduces the expression levels of HIF-1 target genes CA9, ANGPTL4 and EGLN3 and meanwhile reduces the tumor weight. In addition, BAY 87-2243 is also found to act as an inhibitor of mitochondrial function. It can inhibit the oxygen consumption with IC50 value of 10nM [1].

References:
[1] Ellinghaus P, Heisler I, Unterschemmann K, 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. Cancer medicine, 2013, 2(5): 611-624.