GLPBio

PKI-402

Catalog No.: GC17104Purity:>99.50%
COASDSData Sheet

PI3K inhibitor,selective, reversible and ATP-competitive

Products are for research use only. Not for human use. We do not sell to patients.

PKI-402
Cas No.: 1173204-81-3
1mgIn Stock
$25.00
1
5mgIn Stock
$58.00
1
10mgIn Stock
$94.00
1
25mgIn Stock
$188.00
1
50mgIn Stock
$286.00
1
100mgIn Stock
$413.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citations

1 publicationsPublications from researchers using this product

Description

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.

Protocol

Kinase experiment:

Enzyme assays are done in fluorescent polarization (FP) format. Human class I PI3Ks and PI3K-α mutants (E545K and H1047R) are produced in Sf9. GST-GRP1 (murine) is produced in Escherichia coli and isolated by GST-Sepharose. Assay buffers are reaction buffer [20 mM HEPES (pH 7.1), 2 mM MgCl2, 0.05% CHAPS, and 0.01% β-mercaptoethanol] and stop/detection buffer [100 mM HEPES (pH 7.5), 4 mM EDTA, 0.05% CHAPS]. FP reaction is run for 30 min at room temperature in 20 μL of reaction buffer containing 20 μM phosphatidylinositol 4,5-bisphosphate (PIP2), 25 μM ATP, and

Cell experiment:

MDA-MB-361, MDA-MB-468, T47D, MCF7, BT474, HT29, HCT116, DLD1, U87MG, H157, NCI-H460, A549, NCI-H1975, NCI-H1650, NCI-H2170, KB, 786-0, A498, MIA-PaCa-2, and PC3 cell lines are propagated at 37°C in 5% CO2 incubators in supplier-recommended growth medium. Cell growth inhibition is determined using the CellTiter 96 AQueous proliferation assay. Data are collected after 72 h using a Wallac Victor2 V 1420 multilabel HTS counter. FOXO-GFP translocation in U2OS cells is quantified after 60-min PKI-402 exposure using a Cellomics ArrayScan VTI Reader[1].

Animal experiment:

Mice[1]PKI-402 or vehicle is administered by i.v. route. Nude mice bearing MDA-MB-361 tumors are used. Tumor weight is calculated. Pharmacodynamic (biomarker) measurements are done on tumor-bearing female nude mice administered PKI-402. Tumor or normal tissue samples are collected from euthanized animals, homogenized, washed twice with cold (4°C) PBS, and then treated with cell lysis buffer[1].

References:

[1]. Mallon R 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.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1173204-81-3
Chemical Name
1-[4-(3-ethyl-7-morpholin-4-yltriazolo[4,5-d]pyrimidin-5-yl)phenyl]-3-[4-(4-methylpiperazine-1-carbonyl)phenyl]urea
SMILES
CCN1C2=C(C(=NC(=N2)C3=CC=C(C=C3)NC(=O)NC4=CC=C(C=C4)C(=O)N5CCN(CC5)C)N6CCOCC6)N=N1
Molecular Formula
C29H34N10O3
Molecular Weight
570.65
Solubility
≥ 14.275mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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