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AZD6482 PI3K inhibitor

Name: AZD6482
Brand: Selleck Chemicals
SKU: S1462
Availability: InStock
Rating: 5 (27 reviews)

Cat.No.S1462

AZD6482 (KIN-193) is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Phase 1.

Chemical Structure

Molecular Weight: 408.45

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Quality Control

Batch: Purity: 99.92%

99.92

Related Targets	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Other PI3K Inhibitors	LY294002 Buparlisib (BKM120) SAR405 Eganelisib (IPI-549) XL147 analogue Paxalisib (GDC-0084) Tersolisib (STX-478) 3-Methyladenine (3-MA) Dactolisib (BEZ235) Pictilisib (GDC-0941)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
human RXF393 cell	Growth inhibition assay	Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.01154 μM
human SW982 cell	Growth inhibition assay	Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.03584 μM
human MAD-MB-468 cells	Function assay	Inhibition of PI3Kbeta in human MAD-MB-468 cells assessed as inhibition of Ser473 Akt phosphorylation by cellular potency assay, IC50=0.04 μM
human KURAMOCHI cell	Growth inhibition assay	Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=0.1051 μM
human A498 cell	Growth inhibition assay	Inhibition of human A498 cell growth in a cell viability assay, IC50=0.11795 μM
human YT cell	Growth inhibition assay	Inhibition of human YT cell growth in a cell viability assay, IC50=0.12066 μM
human VMRC-RCZ cell	Growth inhibition assay	Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50=0.14898 μM
human MDA-MB-415 cell	Growth inhibition assay	Inhibition of human MDA-MB-415 cell growth in a cell viability assay, IC50=0.16732 μM
human J82 cell	Growth inhibition assay	Inhibition of human J82 cell growth in a cell viability assay, IC50=0.47779 μM
human SW1710 cell	Growth inhibition assay	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=0.5292 μM
human T47D cell	Growth inhibition assay	Inhibition of human T47D cell growth in a cell viability assay, IC50=0.5327 μM
human SU-DHL-1 cell	Growth inhibition assay	Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=0.56813 μM
human BT-20 cell	Growth inhibition assay	Inhibition of human BT-20 cell growth in a cell viability assay, IC50=0.59222 μM
human OS-RC-2 cell	Growth inhibition assay	Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=0.62388 μM
human RPMI-6666 cell	Growth inhibition assay	Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=0.64379 μM
human OVCAR-3 cell	Growth inhibition assay	Inhibition of human OVCAR-3 cell growth in a cell viability assay, IC50=0.67946 μM
human NALM-6 cell	Growth inhibition assay	Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=0.70465 μM
human RS4-11 cell	Growth inhibition assay	Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=0.73806 μM
human SK-MES-1 cell	Growth inhibition assay	Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50=0.78967 μM
human ES7 cell	Growth inhibition assay	Inhibition of human ES7 cell growth in a cell viability assay, IC50=0.81286 μM
human NCI-H2342 cell	Growth inhibition assay	Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=0.84294 μM
human SCC-9 cell	Growth inhibition assay	Inhibition of human SCC-9 cell growth in a cell viability assay, IC50=0.8577 μM
human EW-7 cell	Growth inhibition assay	Inhibition of human EW-7 cell growth in a cell viability assay, IC50=0.86356 μM
human HH cell	Growth inhibition assay	Inhibition of human HH cell growth in a cell viability assay, IC50=0.96222 μM
human A427 cell	Growth inhibition assay	Inhibition of human A427 cell growth in a cell viability assay, IC50=0.99505 μM
human Daudi cell	Growth inhibition assay	Inhibition of human Daudi cell growth in a cell viability assay, IC50=1.06888 μM
human P30-OHK cell	Growth inhibition assay	Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=1.07138 μM
human HGC-27 cell	Growth inhibition assay	Inhibition of human HGC-27 cell growth in a cell viability assay， IC50=1.1816 μM
human CAMA-1 cell	Growth inhibition assay	Inhibition of human CAMA-1 cell growth in a cell viability assay, IC50=1.2001 μM
human SK-OV-3 cell	Growth inhibition assay	Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=1.20444 μM
human NCI-H1048 cell	Growth inhibition assay	Inhibition of human NCI-H1048 cell growth in a cell viability assay, IC50=1.22579 μM
human MEL-HO cell	Growth inhibition assay	Inhibition of human MEL-HO cell growth in a cell viability assay, IC50=1.24238 μM
human NKM-1 cell	Growth inhibition assay	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=1.28636 μM
human NCI-H650 cel	Growth inhibition assay	Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=1.30076 μM
human HAL-01 cell	Growth inhibition assay	Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=1.30175 μM
human 786-0 cell	Growth inhibition assay	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.31283 μM
human GI-1 cell	Growth inhibition assay	Inhibition of human GI-1 cell growth in a cell viability assay, IC50=1.31808 μM
human Becker cell	Growth inhibition assay	Inhibition of human Becker cell growth in a cell viability assay, IC50=1.36315 μM
human CCF-STTG1 cell	Growth inhibition assay	Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=1.42525 μM
human MC116 cell	Growth inhibition assay	Inhibition of human MC116 cell growth in a cell viability assay, IC50=1.46122 μM
human MDA-MB-468 cell	Growth inhibition assay	Inhibition of human MDA-MB-468 cell growth in a cell viability assay, IC50=1.53736 μM
human NB12 cell	Growth inhibition assay	Inhibition of human NB12 cell growth in a cell viability assay, IC50=1.54842 μM
human LXF-289 cell	Growth inhibition assay	Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.55104 μM
human MFE-296 cell	Growth inhibition assay	Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=1.56836 μM
human SNU-423 cell	Growth inhibition assay	Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=1.57192 μM
human NCI-H2291 cell	Growth inhibition assay	Inhibition of human NCI-H2291 cell growth in a cell viability assay, IC50=1.5761 μM
human OCUB-M cell	Growth inhibition assay	Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=1.58314 μM
human KU812 cell	Growth inhibition assay	Inhibition of human KU812 cell growth in a cell viability assay, IC50=1.59628 μM
human HuO9 cell	Growth inhibition assay	Inhibition of human HuO9 cell growth in a cell viability assay, IC50=1.6128 μM
human 639-V cell	Growth inhibition assay	Inhibition of human 639-V cell growth in a cell viability assay, IC50=1.63144 μM
human HCC70 cell	Growth inhibition assay	Inhibition of human HCC70 cell growth in a cell viability assay, IC50=1.66146 μM
human SNB75 cell	Growth inhibition assay	Inhibition of human SNB75 cell growth in a cell viability assay, IC50=1.66508 μM
human D-336MG cell	Growth inhibition assay	Inhibition of human D-336MG cell growth in a cell viability assay, IC50=1.6688 μM
human LoVo cell	Growth inhibition assay	Inhibition of human LoVo cell growth in a cell viability assay, IC50=1.73825 μM
human EB2 cell	Growth inhibition assay	Inhibition of human EB2 cell growth in a cell viability assay, IC50=1.75019 μM
human HSC-2 cell	Growth inhibition assay	Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=1.75727 μM
human D-542MG cell	Growth inhibition assay	Inhibition of human D-542MG cell growth in a cell viability assay, IC50=1.85077 μM
human COLO-684 cell	Growth inhibition assay	Inhibition of human COLO-684 cell growth in a cell viability assay, IC50=2.20032 μM
human GDM-1 cell	Growth inhibition assay	Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=2.24206 μM
human SW1088 cell	Growth inhibition assay	Inhibition of human SW1088 cell growth in a cell viability assay, IC50=2.48143 μM
human SF295 cell	Growth inhibition assay	Inhibition of human SF295 cell growth in a cell viability assay, IC50=2.76955 μM
human NCI-H2030 cell	Growth inhibition assay	Inhibition of human NCI-H2030 cell growth in a cell viability assay, IC50=2.90288 μM
human NCI-H1755 cell	Growth inhibition assay	Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=3.27063 μM
human MDA-MB-361 cell	Growth inhibition assay	Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=3.52709 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (200.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (73.45mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	408.45	Formula	C₂₂H₂₄N₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1173900-33-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	KIN-193			Smiles	CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3C(=O)O)N4CCOCC4

Mechanism of Action

Targets/IC₅₀/Ki	PI3Kβ (Cell-free assay) 10 nM PI3Kδ (Cell-free assay) 80 nM DNA-PK (Cell-free assay) 420 nM PI3Kα (Cell-free assay) 870 nM
In vitro	AZD6482 also inhibits PI3Kα, γ, and δ, with IC50 of 80 nM to 1.09 μM, which are significantly lower than its (+)-enantiomer (S-form). This compound is an antiplatelet agent; it blocks platelet activation adhesion/aggregation and promotes platelet disaggregation in assay of washed platelet aggregation (WPA), with an IC50 value of 6 nM. Furthermore, by targeting PI3Kβ, this chemical specifically inhibits thrombosis without interfering with normal haemostasis. Therefore, it is used as an anti-thrombotic drug for the prophylaxis of thrombotic disorders.
Kinase Assay	Assay of PI3K enzyme inhibition
Kinase Assay	The inhibition of PI3Kβ, PI3Kα, PI3Kγ, and PI3Kδ is evaluated in an AlphaScreen based enzyme activity assay using human recombinant enzymes. The assay measures PI3K-mediated conversion of PIP2 to PIP3. Biotinylated PIP3, a GST-tagged pleckstrin homology (PH) domain and the two AlphaScreen beads form a complex that elicits a signal upon laser excitation at 680 nm. The PIP3 formed in the enzyme reaction competes with the biotinylated PIP3 for binding to the PH domain thus reducing the signal with increasing enzyme product. This compound is dissolved in DMSO and added to 384 well plates. PBKβ, PBKα, PBKγ, or PBKδ is added in a Tris buffer (50 mM Tris pH 7.6, 0.05% CHAPS, 5 mM DTT, and 24 mM MgCl₂) and allowed to preincubate with this chemical for 20 minutes prior to the addition of substrate solution containing PIP2 and ATP. The enzyme reaction is stopped after 20 minutes by addition of stop solution containing EDTA and biotin-PIP3, followed by addition of detection solution containing GST-grpl PH and AlphaScreen beads. Plates are left for a minimum of 5 hours in the dark prior to analysis. The final concentration of DMSO, ATP and PIP2 in the assay are, 0.8%, 4 μM, and 40 μM, respectively. IC50 values are calculated according to the equation, y = {a+[(b-a)/(l+(x/IC50)^s)]}, where y = % inhibition; a = 0%; b = 100%; s = the slope of the concentration-response curve; x = this compound concentration.
References	[1] http://www.wipo.int/patentscope/search/en/WO2009093972

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