LY2584702 1082949-67-4

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Molecular Weight: 445.42 LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.

In HCT116 colon cancer cells, LY2584702 inhibits phosphorylation of the S6 ribosomal protein (pS6) with IC50 of 0.1-0.24 μM. LY2584702 has significant synergistic effects when combined with EGFR
inhibitor erlotinib or with the mTOR Inhibitor everolimus.

LY2584702 (12.5 mg/kg BID, demonstrates significant antitumor efficacy
in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.


Protocol(Only for Reference)


Animal Study: [1]

Animal Models	U87MG glioblastoma and HCT116 colon carcinoma xenograft models
Formulation
Dosages	12.5 mg/kg BID
Administration

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)	445.42
Formula	C21H19F4N7
CAS No.	1082949-67-4

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

Chemical Name	4-(4-(4-(4-fluoro-3-(trifluoromethyl)phenyl)-1-methyl-1H-imidazol-2-yl)piperidin-1-yl)-1H-pyrazolo[3,4-d]pyrimidine

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Product Categories : PI3K/Akt/mTOR > S6 Kinase Inhibitor