Glasdegib (PF-04449913) 1095173-27-5

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Molecular Weight:

374.44 Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.

Biological Activity

In vitro microsomal assays, PF-04449913 have high clearance in rat and
low clearance in dog and human, without inhibiting any of the major
cytochrome P450 isoforms.


In rat and dog, PF-04449913 shows high clearance, and good oral bioavailability.



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)	374.44
Formula	C21H22N6O
CAS No.	1095173-27-5

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

Solubility (25°C) *	In vitro	DMSO	47 mg/mL (125.52 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (

Chemical Name	N-[(2R,4R)-2-(1H-benzimidazol-2-yl)-1-methyl-4-piperidinyl]-N'-(4-cyanophenyl)-urea

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Product Categories : Stem Cells & Wnt > Hedgehog/Smoothened Inhibitor