Ro3280 1062243-51-9

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Molecular Weight:

543.61 RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.


Biological Activity


RO3280 shows the strong anti-proliferative activity against lung cancer
cell line H82, colorectal cancer cell HT-29, breast cancer cell
MDA-MB-468, prostate cancer cell PC3 and skin cancer cell A375 with
IC50s of 5, 10, 19, 12 and 70 nM, respectively.


RO3280 displays robust antitumor activity in nude mouse implanted with
HT-29 human colorectal tumors ranging from 72% tumor growth inhibition
when dosed once weekly at 40 mg/kg, to complete tumor regression when
dosed more frequently..


Protocol(Only for Reference)


Animal Study: [1]

Animal Models	Human colorectal cancer xenografts HT-29
Formulation
Dosages	40 mg/kg
Administration	q4d i.v.

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)	543.61
Formula	C27H35F2N7O3
CAS No.	1062243-51-9

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	Ro5203280

Solubility (25°C) *	In vitro	DMSO	100 mg/mL (183.95 mM)
		Water	<1 mg/mL (
		Ethanol	100 mg/mL (183.95 mM)

Chemical Name	Benzamide, 4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-

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Product Categories : Cell Cycle > PLK Inhibitor