AT13148 1056901-62-2

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Molecular Weight: 313.78 AT13148 is an oral, ATP-competitive, Multi-AGC Kinase Inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.

AT13148, as a multi-AGC kinase inhibitor, potently inhibits
proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel
of cancer cell lines with deregulation of PI3K-AKT-mTOR or RAS-RAF
pathways. In PTEN-deficient MES-SA cells, AT13148 also inhibits AKT and
p70S6K signaling.

AT13148 (50 mg/kg p.o.) markedly inhibits the activity of both AKT and
p70S6K AGC kinases, and subsequently exhibits marked antitumor effects
in human tumor xenografts.

In vitro kinase assays	AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme.

Cell Assay: [1]

Cell lines	MES-SA, MES-SA/Dx5, BT474, HCT-116, A549, PC3, SK-BR-3, MCF7, U87MG, MDA-MB-468, DU-145, and SK-OV-3 cell lines
Concentrations	~10 μM
Incubation Time	72 hours or 96 hours
Method	Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay.

Animal Study: [1]

Animal Models	Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts
Formulation	10% DMSO, 1% Tween-20, and 89% saline
Dosages	~50 mg/kg
Administration	p.o.

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)	313.78
Formula	C17H16ClN3O
CAS No.	1056901-62-2

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

Chemical Name	(S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol

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Product Categories : PI3K/Akt/mTOR > Akt Inhibitor