BAY 87-2243 1227158-85-1

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Molecular Weight:

525.53 BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.


Biological Activity


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 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.


Method


To evaluate the cytotoxicity of BAY 87-2243, 2.000 cells of the
respective cell lines are seeded in 96-well plates and cultured in the
appropriate growth medium containing 10% FCS. BAY 87-2243 at various
concentrations is added at 24 h after seeding for additional 48 h and
cell viability is determined using Cell Titer Glow Assay.


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	525.53
Formula	C26H26F3N7O2
CAS No.	1227158-85-1

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	N/A

Solubility (25°C) *	In vitro	DMSO	<1 mg/mL (
		Water	<1 mg/mL (
		Ethanol	8 mg/mL heating (15.22 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	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

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Product Categories : Epigenetics > HIF Inhibitor