AZD-9291 - CAS 1421373-65-0

Catalog Number Size Price Stock Quantity
BP-300113 2.5 g $365 In stock
BP-300113 5 g $629 In stock
Add to cart

AZD-9291 is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. AZD9291 is highly active in preclinical models and is well tolerated in animal models.
AZD 9291 is an irreversible inhibitor of epidermal growth factor receptor (EGFR) sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM). It binds the related IGF1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 µM, respectively).

* Please be kindly noted that our services and products can only be used for research to organizations or companies and not intended for any clinical or individuals.

Molecular Formula
C28H33N7O2
Molecular Weight
499.61

AZD-9291

    • Specification
      • Related CAS
        1421373-66-1 (mesylate)
        Purity
        98%
        Appearance
        White to off-white powder
        Application
        For research used only
        Synonyms
        Mereletinib; AZD9291; AZD 9291; Osimertinib
    • Properties
      • Boiling Point
        N/A
        Density
        1.2±0.1 g/cm3
        InChI Key
        DUYJMQONPNNFPI-UHFFFAOYSA-N
        InChI
        InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32)
        Canonical 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
    • Reference Reading
      • 1.Osimertinib: A Review in T790M-Positive Advanced Non-Small Cell Lung Cancer.
        Lamb YN;Scott LJ Target Oncol. 2017 Aug;12(4):555-562. doi: 10.1007/s11523-017-0519-0.
        Osimertinib (Tagrisso™) is an oral, CNS-active, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that targets EGFR TKI-sensitizing mutations and, crucially, the T790M mutation that often underlies acquired resistance to EGFR TKI therapy. Osimertinib has been approved in numerous countries for use in patients with T790M-positive advanced NSCLC. In the pivotal, international AURA3 trial in patients with T790M-positive advanced NSCLC who had disease progression after EGFR TKI therapy, osimertinib treatment significantly prolonged progression-free survival (PFS; primary endpoint) compared with platinum-pemetrexed therapy at the time of the primary analysis. PFS results were consistent across predefined subgroups of patients, including those with CNS metastases at baseline. There was no difference between treatment groups in overall survival at 26% maturity. Objective response rates (ORRs) and patient-reported outcomes for prespecified symptoms were also significantly improved with osimertinib relative to platinum-pemetrexed, with CNS ORRs in patients with CNS metastases more than twofold higher in the osimertinib than in the platinum-pemetrexed group.
        2.Can we define the optimal sequence of epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of epidermal growth factor receptor-mutant nonsmall cell lung cancer?
        Sun JM;Park K Curr Opin Oncol. 2017 Mar;29(2):89-96. doi: 10.1097/CCO.0000000000000350.
        PURPOSE OF REVIEW: ;The most common mechanism of resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) is acquisition of the T790M gatekeeper mutation. Third-generation EGFR TKIs irreversibly inhibit EGFR mutants (EGFRm), especially T790M, while sparing wild-type EGFR. There are several third-generation EGFR TKIs under development, including osimertinib, CO-1686 (rociletinib), HM61713 (olmutinib), ASP8273, and EGF816. These third-generation EGFR TKIs have shown promising efficacy with favorable toxicity profiles in the management of advanced nonsmall cell lung cancer (NSCLC) with an acquired T790M mutation (EGFR). In the present review, we will discuss the evolving treatment landscape of EGFRm NSCLC.;RECENT FINDINGS: ;The LUX-Lung 7 study demonstrated superior progression-free survival, time-to-treatment failure, and objective response rate with afatinib versus gefitinib, but no significant overall survival improvement in TKI-naïve EGFRm NSCLC patients. In EGFRm NSCLC patients harboring T790M after treatment with first-generation or second-generation EGFR TKIs, third-generation EGFR TKIs showed robust efficacy with tolerable toxicity. The updated results of phase I studies have demonstrated encouraging activity of first-line osimertinib in patients with EGFRm NSCLC.
        3.Second-Line Treatment of Non-Small Cell Lung Cancer: Clinical, Pathological, and Molecular Aspects of Nintedanib.
        Corrales L;Nogueira A;Passiglia F;Listi A;Caglevic C;Giallombardo M;Raez L;Santos E;Rolfo C Front Med (Lausanne). 2017 Feb 28;4:13. doi: 10.3389/fmed.2017.00013. eCollection 2017.
        Lung carcinoma is the leading cause of death by cancer in the world. Nowadays, most patients will experience disease progression during or after first-line chemotherapy demonstrating the need for new, effective second-line treatments. The only approved second-line therapies for patients without targetable oncogenic drivers are docetaxel, gemcitabine, pemetrexed, and erlotinib and for patients with target-specific oncogenes afatinib, osimertinib, crizotinib, alectinib, and ceritinib. In recent years, evidence on the role of antiangiogenic agents have been established as important and effective therapeutic targets in non-small cell lung cancer (NSCLC). Nintedanib is a tyrosine kinase inhibitor targeting three angiogenesis-related transmembrane receptors (vascular endothelial growth factor, fibroblast growth factor, and platelet-derived growth factor). Several preclinical and clinical studies have proven the usefulness of nintedanib as an anticancer agent for NSCLC. The most important study was the phase III LUME-Lung 1 trial, which investigated the combination of nintedanib with docetaxel for second-line treatment in advanced NSCLC patients. The significant improvement in overall survival and the manageable safety profile led to the approval of this new treatment in Europe.
    • Preparing Stock Solutions
      • ConcentrationVolumeMass1 mg5 mg10 mg
        1 mM2.0016 mL10.0078 mL20.0156 mL
        5 mM0.4003 mL2.0016 mL4.0031 mL
        10 mM0.2002 mL1.0008 mL2.0016 mL
        50 mM0.0400 mL0.2002 mL0.4003 mL
Bio Calculators
Stock concentration: *
Desired final volume: *
Desired concentration: *

L

* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2

* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
g/mol
g
Related Products
BOC Sciences Support

Please contact us with any specific requirements and we will get back to you as soon as possible.


  • Verification code

We invite you to contact us at or through our contact form above for more information about our services and products.

USA
  • International:
  • US & Canada (Toll free):
  • Email:
  • Fax:
UK
  • Email:
Inquiry Basket