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BAY 87-2243

Cat. No. M4869
BAY 87-2243 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 105  USD105 In stock
2mg USD 55  USD55 In stock
5mg USD 82  USD82 In stock
10mg USD 120  USD120 In stock
50mg USD 540  USD540 In stock
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Quality Control & Documentation
Biological Activity

BAY87-2243 is a potent inhibitor of selective hypoxia-inducible facin-1 (HIF-1). Bay87-2243 induces iron death and necrosis in BRAFV600E melanoma cells by inhibiting the mitochondrial respiratory chain, resulting in ROS accumulation, lipid peroxidation, and GSH deletion.

Product Citations
Chemical Information
Molecular Weight 525.53
Formula C26H26F3N7O2
CAS Number 1227158-85-1
Solubility (25°C) DMSO 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Linda Helbig, et al. Radiat Oncol. BAY 87-2243, a novel inhibitor of hypoxia-induced gene activation, improves local tumor control after fractionated irradiation in a schedule-dependent manner in head and neck human xenografts

[2] Ellinghaus P, et.al. Cancer Med. BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I.

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