KPT-185 1333151-73-7

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Molecular Weight:

355.31 KPT-185 is a Selective CRM1 Inhibitor.

Biological Activity

KPT-185 significantly inhibits leukemia cell proliferation with IC50
ranging from 100 nM to 500 nM, and induces cell-cycle arrest and
Apoptosis of AML cell lines and primary AML blasts. KPT-185 reduces CRM1
protein protein level and shows a significant nuclear accumulation of
CRM1 cargo Proteins. KPT-185 also inhibits proliferation
and promotes apoptosis of pancreatic cancer cells without affecting
human pancreatic ductal epithelial cells.



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)

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Product Categories : Transmembrane Transporters > CRM1 Inhibitor