AZ20

Name: AZ20
Brand: MedChemExpress
SKU: HY-15557
Rating: 5.0 (11 reviews)

Cat. No.: HY-15557 Purity: 99.40%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AZ20 is a potent and selective inhibitor of ATR with an IC₅₀ of 5 nM, and has 8-fold selectivity against mTOR (IC₅₀=38 nM).

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

AZ20 Chemical Structure

CAS No. : 1233339-22-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 319	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 11 publication(s) in Google Scholar

10 Publications Citing Use of MCE AZ20

: AZ20 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2017 Aug 10;8(8):e2982. [Abstract]; Tumor pieces from M130116 PDXs treated with the vehicle or the RVX2135/AZ20 combination treatment are subjected to western blot analysis.

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ATM ATR

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

AZ20 is a potent and selective inhibitor of ATR with an IC₅₀ of 5 nM, and has 8-fold selectivity against mTOR (IC₅₀=38 nM).

IC₅₀ & Target^[1]

ATR

5 nM (IC₅₀)

mTOR

38 nM (IC₅₀)

PI3Kα

13000 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.7 μM Compound: AZ20	Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 35191694]
HeLa	IC₅₀	0.005 μM Compound: 6, AZ20	Inhibition of ATR in human HeLa cell nuclear extracts using glutathione S-transferase-p53N66 and ATP as substrate incubated for 10 mins prior to ATP addition measured after 1 hr by ELISA Inhibition of ATR in human HeLa cell nuclear extracts using glutathione S-transferase-p53N66 and ATP as substrate incubated for 10 mins prior to ATP addition measured after 1 hr by ELISA	[PMID: 23394205]
HT-29	IC₅₀	0.05 μM Compound: 6, AZ20	Inhibition of ATR-mediated CHK1 phosphorylation at serine 345 in human HT29 cells after 1 hr in presence of 4-nitroquinoline 1-oxide Inhibition of ATR-mediated CHK1 phosphorylation at serine 345 in human HT29 cells after 1 hr in presence of 4-nitroquinoline 1-oxide	[PMID: 23394205]
HT-29	GI₅₀	0.97 μM Compound: 1; AZ20	Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay	[PMID: 30346772]
LoVo	GI₅₀	0.2 μM Compound: 1; AZ20	Cytotoxicity against human LoVo cells after 72 hrs by MTS assay Cytotoxicity against human LoVo cells after 72 hrs by MTS assay	[PMID: 30346772]
LoVo	GI₅₀	0.2 μM Compound: 6, AZ20	Growth inhibition of human LoVo cells after 72 hrs by MTS assay Growth inhibition of human LoVo cells after 72 hrs by MTS assay	[PMID: 23394205]

In Vitro

AZ20 inhibits ATR immunoprecipitated from HeLa nuclear extracts with an IC₅₀ of 5 nM and ATR mediated phosphorylation of Chk1 in HT29 colorectal adenocarcinoma tumor cells with an IC₅₀ of 50 nM^[1].

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

In Vivo

AZ20 (25, 50 mg/kg, p.o.) has high permeability combined with good stability to rat hepatocytes and, despite the lack of progress in achieving markedly higher solubility, has respectable bioavailability in a low dose rat PK study. AZ20 (25, 50 mg/kg, p.o.) leads to significant tumor growth inhibition in female nude mice bearing LoVo tumors^[1].

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

Molecular Weight

412.51

Formula

C₂₁H₂₄N₄O₃S

CAS No.

1233339-22-4

Appearance

Solid

Color

White to off-white

SMILES

O=S(C1(C2=CC(N3[C@H](C)COCC3)=NC(C4=CC=CC5=C4C=CN5)=N2)CC1)(C)=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 : ≥ 100 mg/mL (242.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4242 mL	12.1209 mL	24.2418 mL
5 mM	0.4848 mL	2.4242 mL	4.8484 mL
10 mM	0.2424 mL	1.2121 mL	2.4242 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 (6.06 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.06 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

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.

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: 99.40%

Select Batch:

Data Sheet (284 KB) SDS (392 KB)

COA (259 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

References

[1]. Foote KM, et al. Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. J Med Chem. 2013 Mar 14 [Content Brief]

Cell Assay ^[1]	Compound dose ranges are created by diluting in 100% DMSO and then further into assay medium (EMEM, 10% FCS, 1% glutamine) using a Labcyte Echo acoustic dispensing instrument. Cells are plated in 384-well Costar plates at 9×10⁴ cells per mL in 40 μL of EMEM, 10% FCS, 1% glutamine and grown for 24 h. Following addition of compound the cells are incubated for 60 min. A final concentration of 3 μM 4NQO (prepared in 100% DMSO) is then added using the Labcyte Echo, and the cells are incubated for a further 60 min. The cells are fixed by adding 40 μL of 3.7% v/v formaldehyde solution for 20 min. After removal of fix, cells are washed with PBS and permeabilized in 40 μL of PBS containing 0.1% Triton X-100. The cells are then washed, and 15 μL primary antibody solution (pChk1 Ser345) is added. The plates are incubated at 4°C overnight. The primary antibody is then washed off, and 20 μL of secondary antibody solution and 1 μM Hoechst 33258 added for 90 min at room temperature. The plates are washed and left in 40 μL of PBS. Plates are then read on an ArrayScan VTI instrument to determine staining intensities, and dose responses are obtained and used to determine the IC₅₀ values for the compounds. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Female Swiss nu/nu mice are housed in negative pressure isolators. LoVo tumor xenografts are established in 8- to 12-week-old mice by injecting 1×10⁷ tumor cells subcutaneously (100 μL in serum free medium) on the left dorsal flank. Animals are randomized into treatment groups when tumors become palpable. AZ20 is prepared in 10% DMSO/40% propylene glycol/50% water and administered orally. Tumors are measured up to three times per week with calipers. Tumor volumes are calculated and the data plotted using the geometric mean for each group versus time. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Foote KM, et al. Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. J Med Chem. 2013 Mar 14 [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.4242 mL	12.1209 mL	24.2418 mL	60.6046 mL
	5 mM	0.4848 mL	2.4242 mL	4.8484 mL	12.1209 mL
	10 mM	0.2424 mL	1.2121 mL	2.4242 mL	6.0605 mL
	15 mM	0.1616 mL	0.8081 mL	1.6161 mL	4.0403 mL
	20 mM	0.1212 mL	0.6060 mL	1.2121 mL	3.0302 mL
	25 mM	0.0970 mL	0.4848 mL	0.9697 mL	2.4242 mL
	30 mM	0.0808 mL	0.4040 mL	0.8081 mL	2.0202 mL
	40 mM	0.0606 mL	0.3030 mL	0.6060 mL	1.5151 mL
	50 mM	0.0485 mL	0.2424 mL	0.4848 mL	1.2121 mL
	60 mM	0.0404 mL	0.2020 mL	0.4040 mL	1.0101 mL
	80 mM	0.0303 mL	0.1515 mL	0.3030 mL	0.7576 mL
	100 mM	0.0242 mL	0.1212 mL	0.2424 mL	0.6060 mL

AZ20 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:

AZ201233339-22-4AZ 20AZ-20ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedInhibitorinhibitorinhibit

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AZ20

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AZ20 Related Antibodies

10 Publications Citing Use of MCE AZ20

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AZ20 Related Antibodies

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Complete Stock Solution Preparation Table

AZ20 Related Classifications

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