AZD-1390 free base · Synonyms: Elrelesertib

AZD1390 is a potent and selective inhibitor of ATM in cells.

For research use only. Not for human or veterinary use.

Target ATM/ATR Apoptosis Checkpoint Kinase (Chk)

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

AZD-1390 structure

CAS No.: 2089288-03-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 420.00	BP-01968-100mg	In stock	Get quote
250 mg	USD 720.00	BP-01968-250mg	In stock	Get quote
500 mg	USD 1,120.00	BP-01968-500mg	In stock	Get quote
1 g	USD 1,620.00	BP-01968-1g	In stock	Get quote
5 g	Inquire	BP-01968-5g	Inquire	Inquire

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Description

AZD1390 is a potent and selective inhibitor of ATM in cells (IC50 = 0.78 nM) with the ability to cross the blood-brain barrier. AZD1390 has >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases. AZD1390 displays excellent oral bioavailability in preclinical species (66% in rat and 74% in dog), is not a substrate for human efflux transporters, and has been shown to efficiently cross the BBB in non-human primate PET studies.

Biological activity

In vitro ATM autophosphorylation inhibition by AZD1390 occurred at 4 hours after treatment, and 3 nM produced strong inhibition of ATM in LN18 GBM cells. Other DDR inhibitors tested under the same conditions at relevant IC50 concentrations did not affect pATM levels. A dose-dependent increase in G2 accumulation occurred after 24 hours following AZD1390 and irradiation at 2 Gy indicative of cells not arresting in S and accumulating in G2 or experiencing problems during mitosis. In vivo In in vivo syngeneic and patient-derived glioma as well as orthotopic lung-brain metastatic models, AZD1390 dosed in combination with daily fractions of IR (whole-brain or stereotactic radiotherapy) significantly induced tumor regressions and increased animal survival compared to IR treatment alone.

Identifiers

SMILES: CC(C)N1C(=O)N(C)C2=C1C1=CC(C3=CC=C(OCCCN4CCCCC4)N=C3)=C(F)C=C1N=C2
InChIKey: VQSZIPCGAGVRRP-UHFFFAOYSA-N

Specifications

MW (average): 477.5737
Formula: C₂₇H₃₂FN₅O₂
CAS No.: 2089288-03-7
Physical state: Solid
Color: White to off-white
Shipping: 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: Powder -20℃ 2 years; 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Durant ST, et al. The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models. Science advances. 2018 Jun;4(6):eaat1719.

[2]. Jucaite A, et al. Brain exposure of the ATM inhibitor AZD1390 in humans-a positron emission tomography study. Neuro-oncology. 2021 Apr 12;23(4):687-696.

[3]. Özdemir D, et al. AZD1390, an Ataxia telangiectasia mutated inhibitor, enhances cisplatin mediated apoptosis in breast cancer cells. Experimental cell research. 2025 Jan 15;444(2):114382.

Same target

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Same research area

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