AZD0156 | AZD-0156 | CAS#1821428-35-6 | ATM inhibitor

MedKoo Cat#: 206501 | Name: AZD0156

Description:

WARNING: This product is for research use only, not for human or veterinary use.

AZD0156 is an orally bioavailable ataxia telangiectasia mutated (ATM) kinase inhibitor, with potential chemo-/radio-sensitizing and antineoplastic activities. Upon oral administration, AZD0156 targets and binds to ATM, thereby inhibiting the kinase activity of ATM and ATM-mediated signaling. This prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. In addition, AZD0156 sensitizes tumor cells to chemo- and radiotherapy.

Chemical Structure

AZD0156

CAS#1821428-35-6

Theoretical Analysis

MedKoo Cat#: 206501

Name: AZD0156

CAS#: 1821428-35-6

Chemical Formula: C26H31N5O3

Exact Mass: 461.2427

Molecular Weight: 461.57

Elemental Analysis: C, 67.66; H, 6.77; N, 15.17; O, 10.40

Price and Availability

Size	Price	Availability
10mg	USD 150.00	Ready to ship
25mg	USD 265.00	Ready to ship
50mg	USD 425.00	Ready to ship
100mg	USD 725.00	Ready to ship
200mg	USD 1,250.00	Ready to ship
500mg	USD 2,450.00	Ready to ship
1g	USD 3,650.00	Ready to ship
2g	USD 5,850.00	Ready to ship

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Related CAS #

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Synonym

AZD0156; AZD-0156; AZD 0156.

IUPAC/Chemical Name

8-[6-[3-(dimethylamino)propoxy]-3-pyridyl]-3-methyl-1-tetrahydropyran-4-yl-imidazo[4,5-c]quinolin-2-one

InChi Key

AOTRIQLYUAFVSC-UHFFFAOYSA-N

InChi Code

InChI=1S/C26H31N5O3/c1-29(2)11-4-12-34-24-8-6-19(16-28-24)18-5-7-22-21(15-18)25-23(17-27-22)30(3)26(32)31(25)20-9-13-33-14-10-20/h5-8,15-17,20H,4,9-14H2,1-3H3

SMILES Code

O=C(N1C2CCOCC2)N(C)C3=C1C4=CC(C5=CC=C(OCCCN(C)C)N=C5)=CC=C4N=C3

Appearance

White to off-white solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A8T05K21

QC Data

View QC data: current batch, Lot#A8T05K21

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

AZD0156 is an ATM inhibitor with an IC50 of 0.58 nM.

In vitro activity:

In FaDu WT cells, AZD0156 inhibited irradiation-induced ATM signaling in a dose-dependent manner as measured by auto-phosphorylation on serine 1981 of ATM, and phosphorylation of ATM substrates including KAP1, RAD50, and CHK2 (Fig. 1A). AZD0156 did not modulate DNA-PKcs phosphorylation following irradiation, indicating that AZD0156 selectively abrogates ATM signaling (Fig. 1A). Reference: Mol Cancer Ther. 2020 Jan;19(1):13-25. https://mct.aacrjournals.org/content/19/1/13.long

In vivo activity:

In Pkd1RC/RC mice, AZD0156 reduced renal cell proliferation, measured by Ki-67, compared to vehicle (Figure 4A,B). In contrast, although the DNA damage marker γ-H2AX was not different between treatment groups (Figure 4A,C), AZD0156 increased renal p53 (Figure 4D,E). Due to the essential role of ATM in apoptosis, cleaved caspase-3 (Asp175) was also investigated. Cleaved-caspase-3 was expressed in distal tubules but was not altered by AZD0156 (Figure 4A). Furthermore, due to the short duration of this study, as expected, no changes in kidney enlargement and percentage cyst area were observed following AZD0156 treatment (Figure 5). Reference: Cells. 2021 Mar; 10(3): 532. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8000896/

	Solvent	mg/mL	mM
Solubility
	DMSO	2.2	4.66
	Ethanol	2.0	4.33

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 461.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Zhang JQJ, Saravanabavan S, Rangan GK. Effect of Reducing Ataxia-Telangiectasia Mutated (ATM) in Experimental Autosomal Dominant Polycystic Kidney Disease. Cells. 2021 Mar 3;10(3):532. doi: 10.3390/cells10030532. PMID: 33802342; PMCID: PMC8000896. 2. Riches LC, Trinidad AG, Hughes G, Jones GN, Hughes AM, Thomason AG, Gavine P, Cui A, Ling S, Stott J, Clark R, Peel S, Gill P, Goodwin LM, Smith A, Pike KG, Barlaam B, Pass M, O'Connor MJ, Smith G, Cadogan EB. Pharmacology of the ATM Inhibitor AZD0156: Potentiation of Irradiation and Olaparib Responses Preclinically. Mol Cancer Ther. 2020 Jan;19(1):13-25. doi: 10.1158/1535-7163.MCT-18-1394. Epub 2019 Sep 18. PMID: 31534013.

In vitro protocol:

In vivo protocol: