[CAS NO. 2089288-03-7] AZD1390
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PRODUCTS SPECIFICATIONS [2089288-03-7]
Store
Catalog
SLK-S8680
Brand
Selleck
CAS
2089288-03-7
DESCRIPTION [2089288-03-7]
Overview
| MDL | MFCD31619275 |
|---|---|
| Molecular Weight | 477.57 |
| Molecular Formula | C27H32FN5O2 |
| SMILES | O=C(N1C(C)C)N(C)C2=C1C3=CC(C4=CC=C(OCCCN5CCCCC5)N=C4)=C(F)C=C3N=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0939 mL | 10.4697 mL | 20.9393 mL |
| 5 mM | 0.4188 mL | 2.0939 mL | 4.1879 mL |
| 10 mM | 0.2094 mL | 1.0470 mL | 2.0939 mL |
| 50 mM | 0.0419 mL | 0.2094 mL | 0.4188 mL |
Description
AZD1390 is a first-in-class orally available and CNS penetrant inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.
Targets
| ATM [1] (Cell-based assay) |
| 0.78 nM |
In vitro
AZD1390 blocks ATM-dependent DDR (DNA damage response) pathway activity and combines with radiation to induce G2 cell cycle phase accumulation, micronuclei, and apoptosis. AZD1390 radiosensitizes glioma and lung cancer cell lines, with p53 mutant glioma cells generally being more radiosensitized than wild type. AZD1390 results in increased genome instability.
In vivo
AZD1390 displays excellent oral bioavailability in preclinical species (66% in rat and 74% in dog). It can efficiently cross the BBB in non-human primate PET studies. Profound tumor regressions and increased animal survival (>50 days) have been observed in orthotopic xenograft models of brain cancer following just 2 or 4 days combination treatment of AZD1390 with radiotherapy, compared to radiotherapy treatment alone. 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 induces tumor regressions and increased animal survival compared to IR treatment alone. AZD1390 has favorable physical, chemical, PK, and PD properties suitable for clinical applications that require exposures within the central nervous system.
References
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