PKI-402

Name: PKI-402
Brand: MedChemExpress
SKU: HY-10683
Rating: 5.0 (11 reviews)

Cat. No.: HY-10683 Purity: 99.17%: Data Sheet
COA

SDS
Handling Instructions
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PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC₅₀=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).

For research use only. We do not sell to patients.

CAS No. : 1173204-81-3

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5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of PKI-402:

PK_i-402 (Standard) Get quote

11 Publications Citing Use of MCE PKI-402

Flow Cytometry

: PKI-402 purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2019 May;52(3):e12609. [Abstract]; Huh7 cells were treated with 8 μg/mL cisplatin and/or 5 μmol/L PKI‐402 in the presence or absence of 5 μmol/L E‐64 for 24 h and then stained with MitoSOX Red and detected using flow cytometry.

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mTOR mTORC1 mTORC2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC₅₀=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).

IC₅₀ & Target^[1]

PI3Kα

2 nM (IC₅₀)

PI3Kα-H1047R

3 nM (IC₅₀)

PI3Kα-E545K

3 nM (IC₅₀)

PI3Kβ

7 nM (IC₅₀)

PI3Kδ

14 nM (IC₅₀)

PI3Kγ

16 nM (IC₅₀)

mTOR

3 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-361	IC₅₀	10 nM Compound: 77	Cytotoxicity against human MDA-MB-361 cells Cytotoxicity against human MDA-MB-361 cells	[PMID: 25387153]
MDA-MB-361	IC₅₀	5 nM Compound: 3, PKI-402	Inhibition of Akt T308 phosphorylation in human MDA-MB-361 cells after 4 hrs by Western blotting Inhibition of Akt T308 phosphorylation in human MDA-MB-361 cells after 4 hrs by Western blotting	[PMID: 19968288]
MDA-MB-361	IC₅₀	8 nM Compound: 2, PKI-402	Growth inhibition of human MDA-MB-361 cells after 72 hrs Growth inhibition of human MDA-MB-361 cells after 72 hrs	[PMID: 21763134]
MDA-MB-361	IC₅₀	8 nM Compound: 3, PKI-402	Cytotoxicity against human MDA-MB-361 cells with Her2+/PI3KCA mutant after 72 hrs Cytotoxicity against human MDA-MB-361 cells with Her2+/PI3KCA mutant after 72 hrs	[PMID: 19968288]
PC-3	IC₅₀	21 nM Compound: 2, PKI-402	Growth inhibition of human PC3 cells after 72 hrs Growth inhibition of human PC3 cells after 72 hrs	[PMID: 21763134]
PC-3	IC₅₀	21 nM Compound: 3, PKI-402	Cytotoxicity against human PC3 cells with PTEN mutant after 72 hrs Cytotoxicity against human PC3 cells with PTEN mutant after 72 hrs	[PMID: 19968288]
Sf9	IC₅₀	1 nM Compound: 2, PKI-402	Inhibition of human PI3Kalpha expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay Inhibition of human PI3Kalpha expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay	[PMID: 21763134]
Sf9	IC₅₀	9 nM Compound: 2, PKI-402	Inhibition of human PI3Kgamma expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay Inhibition of human PI3Kgamma expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay	[PMID: 21763134]

In Vitro

PKI-402 is an equipotent inhibitor of class I PI3K, including the E545K and H1047R PI3K-α mutants (IC₅₀=2, 3 and 3 nM for PI3Kα, PI3Kα-H1047R and PI3Kα-E545K, respectively). PKI-402 causes in vitro growth inhibition of human tumor cell lines derived from a diverse set of human tumor tissues, including breast, brain (glioma), pancreas, and non-small cell lung cancer (NSCLC) tissues. PKI-402 inhibits MDA-MB-361 [breast: Her2⁺ and PIK3CA mutant (E545K)], with an IC₅₀ of 6 nM. PKI-402 inhibits HCT116 (K-Ras and PIK3CA mutant) with an IC₅₀ of 33 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PKI-402 displays antitumor activity (i.v. route) in breast [MDA-MB-361: Her2⁺ and PIK3CA (E545K)], glioma (U87MG and PTEN), and NSCLC (A549; K-Ras and STK11) xenograft models. PKI-402 causes regression in the MDA-MB-361 xenograft model. PKI-402 effect is most pronounced at 100 mg/kg (daily for 5 days, one round), which reduces initial tumor volume and prevents tumor re-growth for 70 days. In MDA-MB-361 tumor tissue, PKI-402 at 100 mg/kg (single dose) fully suppresses p-Akt at both the T308 and the S473 sites at 8 hours and induces cleaved PARP. At 24 hours, p-Akt suppression is still evident, as is cleaved PARP^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

570.65

Formula

C₂₉H₃₄N₁₀O₃

CAS No.

1173204-81-3

Appearance

Solid

Color

White to off-white

SMILES

CCN1N=NC2=C1N=C(N=C2N3CCOCC3)C4=CC=C(C=C4)NC(NC5=CC=C(C=C5)C(N6CCN(CC6)C)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL (8.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7524 mL	8.7619 mL	17.5239 mL
5 mM	0.3505 mL	1.7524 mL	3.5048 mL
10 mM	---	---	---

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 1.43 mg/mL (2.51 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.17%

Select Batch:

Data Sheet (278 KB) SDS (536 KB)

COA (246 KB) HNMR (133 KB) RP-HPLC (234 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Kinase Assay ^[1]	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 <4% DMSO (compound solvent). FP reaction is stopped with 20 μL of stop/detection buffer (10 nM probe and 40 nM GST-GRP), and after 2 h, data are collected. Selectivity of PKI-402 is evaluated in the 236 human kinase panel at [ATP]=K_m for each enzyme^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7524 mL	8.7619 mL	17.5239 mL	43.8097 mL
DMSO	5 mM	0.3505 mL	1.7524 mL	3.5048 mL	8.7619 mL

PKI-402 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PKI-4021173204-81-3PKI402PKI 402PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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PKI-402

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PKI-402 Related Antibodies

11 Publications Citing Use of MCE PKI-402

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Biological Activity

Protocol

Purity & Documentation

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Customer Review

PKI-402 Related Antibodies

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Complete Stock Solution Preparation Table

PKI-402 Related Classifications

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