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PKI-402

Catalog No.
A8505
PI3K inhibitor,selective, reversible and ATP-competitive
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$270.00
In stock
5mg
$149.00
In stock
10mg
$259.00
In stock
50mg
$679.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

PKI-402 is a selective, equipotent and ATP-competitive class I PI3K inhibitor (IC50= 1 nM, 7 nM, 16 nM and 14 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.)

 

PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt/mTOR pathway.

 

In multiple human cancer cell lines (e.g. breast, brain, pancreas and NSCL), PKI-402 inhibited growth of cancer cells, and attenuated phosphorylation of effector of PI3K and mTOR. In MDA-MB-361, 30 nM PKI-402 caused cleaved of the apoptosis marker—PARP.

 

In MDA-MB-361 mouse tumor xenograft models, administration of 100 mg/kg of PKI-402 daily for 5 days decreased the initial tumor volume from 260 mm3 to 129 mm3 and inhibited tumor regrowth for 70 days, single dose of PKI-402 blocked phosphorylation of Akt and led to cleaved PARP.

 

 

Reference:

 1. Mallon R, Hollander I, Feldberg L et al. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol Cancer Ther. 2010 Apr;9(4):976-84.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt570.65
Cas No.1173204-81-3
FormulaC29H34N10O3
Solubility≥14.275mg/mL in DMSO
Chemical Name1-[4-(3-ethyl-7-morpholin-4-yltriazolo[4,5-d]pyrimidin-5-yl)phenyl]-3-[4-(4-methylpiperazine-1-carbonyl)phenyl]urea
SDFDownload SDF
Canonical SMILESCCN1C2=C(C(=NC(=N2)C3=CC=C(C=C3)NC(=O)NC4=CC=C(C=C4)C(=O)N5CCN(CC5)C)N6CCOCC6)N=N1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description PKI-402 is a potent dual inhibitor of PI3K/mTOR with IC50 values of 2 nM/7 nM/16 nM/14 nM and 3 nM for PI3Kα/β/γ/δ and mTOR, respectively.
Targets PI3Kα mTOR PI3Kβ PI3Kδ PI3Kγ  
IC50 2 nM 3 nM 7 nM 14 nM 16 nM  

Quality Control

Quality Control & MSDS

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Chemical structure

PKI-402