BAY 87-2243

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 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