AZD1208 1204144-28-4

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Molecular Weight:

379.48 AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3, respectively. Phase 1.


Biological Activity


AZD1208 is an orally available, potent and highly selective Pim
inhibitor that effectively inhibits all three isoforms. AZD1208 inhibits
the growth of several AML cell lines and sensitivity correlates with
the level of Pim-1 expression, STAT5 activation and presence of protein
tyrosine kinase mutation.


AZD1208 causes Cell Cycle arrest and Apoptosis
in MOLM-16 cells in culture. This is accompanied by a dose-dependent
reduction in phosphorylation of BAD, 4EBP1 and p70S6K. In addition,
AZD1208 leads to potent inhibition of colony growth of primary AML cells
from bone marrow aspirates and downregulates phosphorylation of Pim
targets.

AZD1208 suppresses the growth of MOLM-16 and KG-1a xenograft tumors in vivo in a dose proportional manner.


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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