AZD1390 - Moligand™, 10mM in DMSO , Inhibitor of ATM serine/threonine kinase, CAS No.2089288-03-7, Inhibitor of ATM serine/threonine kinase

CAS: 2089288-03-7 Cat. No.: A408361 Summenformel: C₂₇H₃₂FN₅O₂ Molekulargewicht: 477.57

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2H-​Imidazo[4,​5-​c]​quinolin-​2-​one, 7-​fluoro-​1,​3-​dihydro-​3-​methyl-​1-​(1-​methylethyl)​-​8-​[6-​[3-​(1-​piperidinyl)​propoxy]​-​3-​pyridinyl]​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

AZD1390 is a first-in-class orally available and CNS penetrantATMinhibitor 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.
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.
Cell Data

cell lines：

Concentrations：0-1250 nM

Incubation Time：1 h

Powder Purity:≥99%

Specifications

Synonyme

2H-​Imidazo[4,​5-​c]​quinolin-​2-​one, 7-​fluoro-​1,​3-​dihydro-​3-​methyl-​1-​(1-​methylethyl)​-​8-​[6-​[3-​(1-​piperidinyl)​propoxy]​-​3-​pyridinyl]​-

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

AZD1390 is a first-in-class orally available and CNS penetrant ATM 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 kina

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Inhibitor of ATM serine/threonine kinase

Produkteigenschaften

• ALogP: 4.231
• hba_count: 4
• Rotationsfähige Bindung: 7

Namen und Kennungen

• Isomere SMILES: CC(C)N1C2=C(C=NC3=CC(=C(C=C32)C4=CN=C(C=C4)OCCCN5CCCCC5)F)N(C1=O)C
• Molekulargewicht: 477.57
• Reaxy-Rn: 31033040
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=31033040&ln=

Zugehörige Ziele (menschlich)

ATM Tchem Serine-protein kinase ATM (1 Activities)

Discover Target: ATM

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (1 Activities)

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemische und physikalische Eigenschaften

• Löslichkeit: Solubility (25°C) In vitro
• DMSO (mg/ml) Maximale Löslichkeit: 14
• DMSO (mM) Maximale Löslichkeit: 29.3150742299558
• Wasser (mg/ml) Maximale Löslichkeit: ＜1