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PKI-402

Cat. No. M3218
PKI-402 Structure
Size Price Availability
5mg USD 170 Out of stock
10mg USD 280 Out of stock
50mg USD 800 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

PKI-402 is a selective, reversible, ATP-competitive, equipotent class I phosphatidylinositol 3-kinases (PI3K) inhibitor with IC50 of 1, 7, 16 and 14 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. PKI-402 gave rise to in vitro growth inhibition of human tumor cell lines derived from breast, brain (glioma), pancreas, and non small cell lung cancer (NSCLC) tissues. In many cases IC50 values were <100 nM. In vitro, PKI-402 suppressed phosphorylation of PI3K and mTOR effect or proteins, particularly p-Akt at threonine308 (T308), at concentrations that closely matched those that inhibited tumor cell growth. In MDA361, a breast tumor line with elevated levels of Her2 receptor, and mutant PI3K- (E545K), 30 nM PKI-402 triggered cleaved PARP, a marker for apoptosis. In vivo, PKI-402 revealed anti-tumor activity when administered by IV route in glioma (U87MG, PTEN), NSCLC (A549; K-Ras, STK11), and breast (MDA361: Her2+, PIK3CA [E545K]) xenograft models. At 25, 50, and 100 mg/kg PKI-402 caused regression of MDA361 tumors. PKI-402 effect was most pronounced at 100 mg/kg (daily for 5 days, 1 round),which decreased an initial tumor volume of 260 mm3 to 129 mm3, and inhibited tumor re-growth for 70 days. Tumor re-growth occurred between days 16-20 when PKI-402 was administered at 25and 50 mg/kg (dx5, 2 rounds). In MDA-MB-361 [breast: Her2 (+) and PIK3CA mutant (E545K)], 30 nM PKI-402 induced cleaved poly (ADP-ribose) polymerase (PARP), a marker for apoptosis.

Protocol
Cell Experiment
Cell lines MDA-MB-361, MDA-MB-468, T47D, MCF7, BT474, HT29, HCT116, DLD1, U87MG, H157, NCI-H460, A549, NCI-H1975, NCI-H1650, NCIH2170, KB, 786-0, A498, MIA-PaCa-2, and PC3
Preparation method Determine cell growth inhibition using the CellTiter 96 Aqueous nonradioactive cell proliferation assay. This homogeneous colorimetric method determined the number of viable cells in proliferation assays. Carry out the assay in 96-well format, with cell number numbers per well being adjusted on the basis of growth characteristics of the various cell lines used. After 72 hours of PKI-402 exposure using a Victor2 V (Wallac) model 1420 multilabel HTS counter, quantify assay end point data .
Concentrations Dissolved in DMSO, final concentrations ~3 μM
Incubation time 72 hours
Animal Experiment
Animal models Female nude mice injected subcutaneously with MDA-361, U87MG, or A549 cells
Formulation Dissolved in 0.5% methylcellulose and 0.4% polysorbate 80 (Tween-80)
Dosages ~100 mg/kg/day
Administration Administered by i.v. route
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 570.65
Formula C29H34N10O3
CAS Number 1173204-81-3
Purity >98%
Solubility DMSO
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PKI-402 supplier, PI3K, inhibitors

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