Osimertinib (AZD9291) - Moligand™, 10mM in DMSO , Epidermal growth factor receptor erbB1 inhibitor, CAS No.1421373-65-0, Epidermal growth factor receptor erbB1 inhibitor

CAS: 1421373-65-0 Cat. No.: O408946 Summenformel: C₂₈H₃₃N₇O₂ Molekulargewicht: 499.62 EG-Nummer: 108-168-8

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Mereletinib | 2-​Propenamide, N-​[2-​[[2-​(dimethylamino)​ethyl]​methylamino]​-​4-​methoxy-​5-​[[4-​(1-​methyl-​1H-​indol-​3-​yl)​-​2-​pyrimidinyl]​amino]​phenyl]​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

Osimertinib (AZD9291) is an oral, irreversible, and mutant-selectiveEGFRinhibitor withIC50of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.
In vitro

AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro.

In vivo

AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo.
Cell Data

cell lines：HUVECs

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyme

Mereletinib | 2-​Propenamide, N-​[2-​[[2-​(dimethylamino)​ethyl]​methylamino]​-​4-​methoxy-​5-​[[4-​(1-​methyl-​1H-​indol-​3-​yl)​-​2-​pyrimidinyl]​amino]​phenyl]​-

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.

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

Epidermal growth factor receptor erbB1 inhibitor

Produkteigenschaften

ALogP

3.7

Namen und Kennungen

Isomere SMILES

CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC

Alternative CAS-Nummer

1421373-65-0

MeSH-Eintrag

AZD-9291;AZD-9291 mesylate;AZD9291;AZD9291 mesylate;mereletinib;mereletinib mesilate;mereletinib mesylate;N-(2-((2-(dimethylamino)ethyl)methylamino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-2-propenamide;N-(2-((2-(dimethylamino

Molekulargewicht

499.62

Reaxy-Rn

23334373

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23334373&ln=

Zugehörige Ziele (menschlich)

ERBB3 Tclin Receptor tyrosine-protein kinase erbB-3 (1 Activities)

Discover Target: ERBB3

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

ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 (1 Activities)

Discover Target: ERBB2

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

EGFR Tclin Epidermal growth factor receptor (92 Activities)

Discover Target: EGFR

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

CARS Tchem Cysteine--tRNA ligase, cytoplasmic (1 Activities)

Discover Target: CARS

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: 51 mg/mL (198.62 mM)

Häufig gestellte Fragen

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1421373-65-0, the molecular formula is C28H33N7O2, and the molecular weight is 499.62 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.