AZD 6482 (Synonyms: KIN-193)

Name: AZD 6482
Brand: MedChemExpress
SKU: HY-10344
Rating: 5.0 (27 reviews)

Cat. No.: HY-10344 Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

AZD 6482 Chemical Structure

CAS No. : 1173900-33-8

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Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 81	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 81	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of AZD 6482:

(S)-AZD 6482 Get quote
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20 Publications Citing Use of MCE AZD 6482

: AZD 6482 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2019 Jan;440-441:54-63. [Abstract]; The cells are transfected with either the negative control (siNC) or BTF3 siRNA for 12 hours followed by BKM-120 or AZD-6482 treatment for 48 hours. The protein abundance is determined by an immunoblotting analysis.

: AZD 6482 purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2019 Jan;41(1):125-132. [Abstract]; The expression levels of Bcl-2, Bax and related proteins of the PI3K signalling pathway are used to assess the inhibitory effect of AZD6482. Each protein is analysed in triplicate, and a representative experiment is shown.

: AZD 6482 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2016 Sep 20;2:16030. [Abstract]; Effects of combined inhibition of PI3K and STAT3 pathways on PTEN-mutated T-ALL cells. (a) Short-term treatment of Ba/F3-shPTEN-NTRK2-Tel cells with isoform-selective inhibitors and Pan-PI3K inhibitor GDC-0032. Cells are treated with DMSO, BYL719, KIN193, GS-1101, GDC-0032 (1 μM) or JAK–STAT inhibitor AZD-1480 (1 μM) for 3 h (n=3) for each treatment. (b) Immunoblot analysis of P-Akt and p-S6 in PF382 and JURKAT cells. Cells are treated with the same inhibitors as in a. (c) Combination of siNTRK2

: AZD 6482 purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jul 7;35(27):3607-12. [Abstract]; (A) Immunoblot analyses in HCC1569 cells treated with BYL719, KIN193 (MedChemexpress) or BKM120 (μM). (B, C) Immunoblot analyses in BT474 and BT474-shPTEN cells treated as indicated in (A).

: AZD 6482 purchased from MedChemExpress. Usage Cited in: Tumour Biol. 2016 Nov;37(11):14831-14839. [Abstract]; Western blot analysis of PI3K signaling in NIC-PTEN^L/L cells treated with BYL719, AZD6482, or BKM120.

: AZD 6482 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2015 Oct 7;6:8501. [Abstract]; Western blot analysis of Akt signalling in whole BM cells at 7 DPI. Freshly isolated BM cells are treated with DMSO, BYL719, KIN193, GS1101 or NVSPI35 at the 1-μM dose for 2 h (n=6) for each treatment.

: AZD 6482 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2012 May;2(5):425-33. [Abstract]; Effects of KIN-193, GDC-0941, PIK-75 and IC87114 on AKT phosphorylation in PTEN-deficient cell lines as indicated. Representative western blots are shown. Bar graphs represent mean ± SD of western blot quantitations of AKTT308 (n=3).

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View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target^[1]

PI3Kβ

0.69 nM (IC₅₀)

PI3Kδ

13.6 nM (IC₅₀)

PI3Kγ

47.8 nM (IC₅₀)

PI3Kα

136 nM (IC₅₀)

PI3K-C2β

54.1 nM (IC₅₀)

hVps34

3390 nM (IC₅₀)

DNA-PK

53.7 nM (IC₅₀)

mTOR

3930 nM (IC₅₀)

PI4Kα

8830 nM (IC₅₀)

Autophagy

Cellular Effect

Cell Line	Type	Value	Description	References
Platelet	IC₅₀	0.27 μM Compound: 2, AZD6482	Antiplatelet activity against human platelet assessed as inhibition of ADP-induced whole blood aggregation by light transmission aggregometry Antiplatelet activity against human platelet assessed as inhibition of ADP-induced whole blood aggregation by light transmission aggregometry	[PMID: 25042253]
Platelet	IC₅₀	1.4 μM Compound: 2, AZD6482	Antiplatelet activity against dog platelet assessed as inhibition of ADP-induced whole blood aggregation by light transmission aggregometry Antiplatelet activity against dog platelet assessed as inhibition of ADP-induced whole blood aggregation by light transmission aggregometry	[PMID: 25042253]
Platelet	IC₅₀	280 nM Compound: 2, AZD6482	Antiplatelet activity against human platelet assessed as inhibition of collagen-induced platelet rich plasma aggregation by light transmission aggregometry Antiplatelet activity against human platelet assessed as inhibition of collagen-induced platelet rich plasma aggregation by light transmission aggregometry	[PMID: 25042253]

In Vitro

An in vitrokinase assay demonstrates that AZD 6482 (KIN-193) is highly potent in the inhibition of p110β’s kinase activity (IC₅₀ of 0.69 nM) and has 200, 20, and 70-fold selectivity over p110α, p110δ, and p110γ isoforms, respectively. AZD 6482 also exhibits selectivity of ~80 fold over PI3K-C2β and DNA-PK and more than 1,000-fold over other phosphatidylinositol-3 kinase–related kinases (PIKKs). An inhibitor-kinase interaction profiling of AZD 6482 against a panel of 433 kinases using the KinomeScan approach demonstrates that AZD 6482 is highly selective in its interaction with PI3Ks. To determine whether AZD 6482 selectively targets PTEN-deficient tumors, the effect of AZD 6482 is tested on cell proliferation on a large panel of 422 cancer cell lines using high-throughput tumor cell line profiling. 35% of cell lines with PTEN mutations (20 out of 57) and 16% of cell lines with wild-type PTEN (58 out of 365) are sensitive to AZD 6482 with a threshold of EC₅₀<5 μM^[1].

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

In Vivo

To determine the pharmacodynamics of AZD 6482 (KIN-193) in tumors in vivo, rat fibroblast (Rat1) cells are engineered to express both p53DD, a dominant negative mutant of p53, and a constitutively activated myr-p110β (Rat1-CA-p110β) to enable these cells to form xenograft tumors in mice. For comparison, an isogenic Rat1 cell line expressing p53DD and myr-p110α (Rat1-CA-p110α) is also generated. Rat1-CA-p110α and Rat1-CA-p110β cells are introduced subcutaneously into the contralateral flanks of athymic mice such that tumors driven by activated p110α or p110β would be exposed to identical conditions and that concern about animal-to-animal variability could be eliminated. When tumors reach a volume of ~500 mm³, the tumor-bearing mice receives a single IP injection of AZD 6482 (10 mg/kg). The plasma concentration of AZD 6482 is highest at 1 hour post-injection and declined to undetectable levels by 4h. Concentrations of AZD 6482 in both the CA-p110α- and CA-p110β-driven tumors parallel the plasma concentrations. Analyses of tumor lysates harvested at various time points after AZD 6482 injection reveal that the phosphorylation of AKT is significantly reduced at 1hour after AZD 6482 injection in Rat1-CA-p110β tumors, but remain unchanged in Rat1-CAp110α tumors^[1].

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

Clinical Trial

Molecular Weight

408.45

Formula

C₂₂H₂₄N₄O₄

CAS No.

1173900-33-8

Appearance

Solid

Color

White to light yellow

SMILES

O=C1N2C(C([C@H](NC3=CC=CC=C3C(O)=O)C)=CC(C)=C2)=NC(N4CCOCC4)=C1

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 : 50 mg/mL (122.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4483 mL	12.2414 mL	24.4828 mL
5 mM	0.4897 mL	2.4483 mL	4.8966 mL
10 mM	0.2448 mL	1.2241 mL	2.4483 mL

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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μL

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (283 KB) SDS (252 KB)

COA (252 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[1]. Ni J, et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2012 May;2(5):425-33. [Content Brief]

Kinase Assay ^[1]	AZD 6482 (KIN-193) is profiled at a concentration of 10 µM against a diverse panel of 433 kinases. Scores for primary screen hits are reported as percent of the DMSO control (% control). For kinases where no score is shown, no measurable binding is detected. The lower the score, the lower the K_d is likely to be, such that scores of zero represent strong hits. Scores are related to the probability of a hit, but are not strictly an affinity measurement. At a screening concentration of 10 µM, a score of less than 10% implies that the false positive probability is less than 20% and the K_d is most likely less than 1 µM. A score between 1-10% implies that the false positive probability is less than 10%, although it is difficult to assign a quantitative affinity from a single-point primary screen. A score of less than 1% implies that the false positive probability is less than 5% and the K_d is most likely less than 1 µM^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cell viability is determined. Briefly, cells are seeded in medium containing 5% FBS at a density insuring cell growth throughout drug treatment (~15% for most cell lines). Drug treatment is started 24 h post seeding and continued for 72 h. Cell are fixed and stained using Syto60, a red fluorescent DNA stain. The relative cell number is calculated by taking the ratio of the relative fluorescence intensity from drug treated wells over untreated wells after background subtraction (cells-free wells). Nine doses of AZD 6482 (KIN-193) are used in 2-fold dilution steps ranging from 5.12 µM to 0.02 µM. IC₅₀, corresponding to 50% cell number compared to control (untreated) wells, is determined using a fixed top and bottom sigmoidal fitting algorithm implemented in PipelinePilot^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Approximately 6-8 week-old female nude mice are injected s.c. with Rat1-Myr-HA-p110α(Rat1-CAp110α) cells (1×10⁶ cells in 40% matrigel) in one flank (site 1) and Rat1-Myr-HA-p110β (Rat1-CAp110β) cells (0.5×10⁶ cells in 10% matrigel) in the contralateral flank (site 2). When tumors grow to ~500 mm³, mice are dosed once by ip injection with AZD 6482 formulated in 7.5% NMP, 40% PEG400, 52.5% dH₂O at 0.1 mL/10g body weight and 10 mg/kg. Tumors are collected at 0, 1, 4, 8, and 24 h following compound administration and blood samples are obtained by direct heart puncture. Serum is separated and stored at -80°C. The drug concentrations in serum and tumor samples are assessed by LC-MS/MS analysis by the DMPK group. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Ni J, et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2012 May;2(5):425-33. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.4483 mL	12.2414 mL	24.4828 mL	61.2070 mL
	5 mM	0.4897 mL	2.4483 mL	4.8966 mL	12.2414 mL
	10 mM	0.2448 mL	1.2241 mL	2.4483 mL	6.1207 mL
	15 mM	0.1632 mL	0.8161 mL	1.6322 mL	4.0805 mL
	20 mM	0.1224 mL	0.6121 mL	1.2241 mL	3.0604 mL
	25 mM	0.0979 mL	0.4897 mL	0.9793 mL	2.4483 mL
	30 mM	0.0816 mL	0.4080 mL	0.8161 mL	2.0402 mL
	40 mM	0.0612 mL	0.3060 mL	0.6121 mL	1.5302 mL
	50 mM	0.0490 mL	0.2448 mL	0.4897 mL	1.2241 mL
	60 mM	0.0408 mL	0.2040 mL	0.4080 mL	1.0201 mL
	80 mM	0.0306 mL	0.1530 mL	0.3060 mL	0.7651 mL
	100 mM	0.0245 mL	0.1224 mL	0.2448 mL	0.6121 mL

AZD 6482 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:

AZD 64821173900-33-8KIN-193AZD6482AZD-6482KIN193KIN 193PI3KAutophagyPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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AZD 6482 (Synonyms: KIN-193)

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20 Publications Citing Use of MCE AZD 6482

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References

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AZD 6482 Related Antibodies

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Complete Stock Solution Preparation Table

AZD 6482 Related Classifications

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