Osimertinib dimesylate - 10mM in Water , CAS No.2070014-82-1

CAS: 2070014-82-1 Cat. No.: O656335 Formula: C₃₀H₄₁N₇O₈S₂ Peso molecolare: 691.82 PubChem CID: 92044416

GRADE & PURITY 10mM in Water

Storage

Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC 50 s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M , respectively.

In Vitro

Osimertinib (AZD-9291) shows similar potency to early generation tyrosine kinase inhibitor (TKIs) in inhibiting EGFR phosphorylation in EGFR cells harboring sensitising EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC 50 values ranging from 13 to 54 nM for Osimertinib (AZD-9291). Osimertinib (AZD-9291) also potently inhibits phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC 50 potency less than 15 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The tumor-bearing mice are treated with Osimertinib (AZD-9291) (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice displays nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib (AZD-9291), while 5 of 5 mice treated with vehicle shows tumor growth . Osimertinib (AZD-9291) demonstrates improved rat PK, reduced hERG affinity, and improved IGF1R margins relative to the previously described compounds, and so this compound is selected for further investigation. Osimertinib (AZD-9291) also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing Osimertinib (AZD-9291) in three efficacy models, The comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib (AZD-9291) is dosed at 5 mg/kg per day. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:EGFR L858R 12 nM (IC 50 ) EGFR L858R/T790M 1 nM (IC 50 )

Specifications

Specifiche e purezza

10mM in Water

Meccanismi biochimici e fisiologici

Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC 50 s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M , respectively.

Condizioni di conservazione di stoccaggio

Desiccated,Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

INHIBITOR

Nomi e identificatori

• Isomeri 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.CS(=O)(=O)O.CS(=O)(=O)O
• PubChem CID: 92044416
• Peso molecolare: 691.82

Domande frequenti

How should this product be stored?

Store at ?80 °C, desiccated. Keep the container tightly closed with desiccant — the material is moisture-sensitive.

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 2070014-82-1, the molecular formula is C30H41N7O8S2, and the molecular weight is 691.82 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.