AZD0156
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MedKoo CAT#: 206501

CAS#: 1821428-35-6

Description: 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

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AZD0156
CAS# 1821428-35-6
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206501
Name: AZD0156
CAS#: 1821428-35-6
Chemical Formula: C26H31N5O3
Exact Mass: 461.24
Molecular Weight: 461.566
Elemental Analysis: C, 67.66; H, 6.77; N, 15.17; O, 10.40

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 265 Ready to ship
50mg USD 425 Ready to ship
100mg USD 725 Ready to ship
200mg USD 1250 Ready to ship
500mg USD 2450 Ready to ship
1g USD 3650 Ready to ship
2g USD 5850 Ready to ship
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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:

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/

Solubility Data

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

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.

Recalculate based on batch purity %
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: 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 vivo 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.

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