AZD6482

PI3Kβ inhibitor,potent and selective CAS# 1173900-33-8

AZD6482

Catalog No. BCC2523----Order now to get a substantial discount!

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Chemical structure

AZD6482

3D structure

Chemical Properties of AZD6482

Cas No. 1173900-33-8 SDF Download SDF
PubChem ID 44137675 Appearance Powder
Formula C22H24N4O4 M.Wt 408.45
Type of Compound N/A Storage Desiccate at -20°C
Synonyms KIN 193
Solubility DMSO : ≥ 100 mg/mL (244.83 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-[[(1R)-1-(7-methyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)ethyl]amino]benzoic acid
SMILES CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3C(=O)O)N4CCOCC4
Standard InChIKey IRTDIKMSKMREGO-OAHLLOKOSA-N
Standard InChI InChI=1S/C22H24N4O4/c1-14-11-17(15(2)23-18-6-4-3-5-16(18)22(28)29)21-24-19(12-20(27)26(21)13-14)25-7-9-30-10-8-25/h3-6,11-13,15,23H,7-10H2,1-2H3,(H,28,29)/t15-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of AZD6482

DescriptionPotent and selective inhibitor of PI 3-kinase β (PI 3-Kβ) (IC50 values are 0.69, 13.6, 47.8 and 136 nM for PI 3-Kβ, PI 3-Kδ, PI 3-Kγ and PI 3-Kα, respectively). Selectively inhibits in vivo growth of the PTEN-deficient tumor xenografts HCC70 and PC3. Also exhibits antithrombotic activity.

AZD6482 Dilution Calculator

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AZD6482 Molarity Calculator

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Preparing Stock Solutions of AZD6482

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4483 mL 12.2414 mL 24.4828 mL 48.9656 mL 61.207 mL
5 mM 0.4897 mL 2.4483 mL 4.8966 mL 9.7931 mL 12.2414 mL
10 mM 0.2448 mL 1.2241 mL 2.4483 mL 4.8966 mL 6.1207 mL
50 mM 0.049 mL 0.2448 mL 0.4897 mL 0.9793 mL 1.2241 mL
100 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.4897 mL 0.6121 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on AZD6482

AZD6428 is a potent, selective and ATP-competitive PI3Kβ inhibitor. IC50 are 0.69, 13.6, 47.8 and 136 nM for PI 3-Kβ, PI 3-Kδ, PI 3-Kγ and PI 3-Kα, 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 vitro, AZD6482 inhibited insulin-activated uptake of human adpocyte glucose (IC50=4.4 μm). A full anti-thrombotic response with no increased bleeding or blood loss was observed in dog treated with AZD6482 in vivo. It also showed good tolerance in a three-hour AZD6482 infusion in healthy volunteers. There was an approx.10-20% rise at 5.3 μm (highest plasma concentration) according to the homeostasis model analysis index. [1]

Reference:
Nylander S, Kull B, Björkman JA et al.  Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor. J Thromb Haemost. 2012 Oct;10(10):2127-36.

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References on AZD6482

Human target validation of phosphoinositide 3-kinase (PI3K)beta: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kbeta inhibitor.[Pubmed:22906130]

J Thromb Haemost. 2012 Oct;10(10):2127-36.

BACKGROUND: Based on in vitro and animal data, PI3Kbeta is given an important role in platelet adhesion and aggregation but its role in insulin signaling is unclear. OBJECTIVE: To strengthen the PI3Kbeta target validation using the novel, short-acting inhibitor AZD6482. METHODS AND RESULTS: AZD6482 is a potent, selective and ATP competitive PI3Kbeta inhibitor (IC(50) 0.01 mum). A maximal anti-platelet effect was achieved at 1 mum in the in vitro and ex vivo tests both in dog and in man. In dog, in vivo AZD6482 produced a complete anti-thrombotic effect without an increased bleeding time or blood loss. AZD6482 was well tolerated in healthy volunteers during a 3-h infusion. The ex vivo anti-platelet effect and minimal bleeding time prolongation in the dog model translated well to data obtained in healthy volunteers. AZD6482 inhibited insulin-induced human adipocyte glucose uptake in vitro (IC(50) of 4.4 mum). In the euglycemic hyperinsulinemic clamp model, in rats, glucose infusion rate was not affected at 2.3 mum but reduced by about 60% at a plasma exposure of 27 mum. In man, the homeostasis model analysis (HOMA) index increased by about 10-20% at the highest plasma concentration of 5.3 mum. CONCLUSIONS: This is the first human target validation for PI3Kbeta inhibition as anti-platelet therapy showing a mild and generalized antiplatelet effect attenuating but not completely inhibiting multiple signaling pathways with an impressive separation towards primary hemostasis. AZD6482 at 'supratherapeutic' plasma concentrations may attenuate insulin signaling, most likely through PI3Kalpha inhibition.

Functional characterization of an isoform-selective inhibitor of PI3K-p110beta as a potential anticancer agent.[Pubmed:22588880]

Cancer Discov. 2012 May;2(5):425-33.

UNLABELLED: Genetic approaches have shown that the p110beta isoform of class Ia phosphatidylinositol-3-kinase (PI3K) is essential for the growth of PTEN-null tumors. Thus, it is desirable to develop p110beta-specific inhibitors for cancer therapy. Using a panel of PI3K isoform-specific cellular assays, we screened a collection of compounds possessing activities against kinases in the PI3K superfamily and identified a potent and selective p110beta inhibitor: KIN-193. We show that KIN-193 is efficacious specifically in blocking AKT signaling and tumor growth that are dependent on p110beta activation or PTEN loss. Broad profiling across a panel of 422 human tumor cell lines shows that the PTEN mutation status of cancer cells strongly correlates with their response to KIN-193. Together, our data provide the first pharmacologic evidence that PTEN-deficient tumors are dependent on p110beta in animals and suggest that KIN-193 can be pursued as a drug to treat tumors that are dependent on p110beta while sparing other PI3K isoforms. SIGNIFICANCE: We report the first functional characterization of a p110beta-selective inhibitor, KIN-193, that is efficacious as an antitumor agent in mice. We show that this class of inhibitor holds great promise as a pharmacologic agent that could be used to address the potential therapeutic benefit of treating p110beta-dependent PTEN-deficient human tumors.

Description

AZD 6482 (KIN-193) is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.

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