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AZD-9291

Basic information Uses Safety Supplier Related

AZD-9291 Basic information

Product Name:
AZD-9291
Synonyms:
  • N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide
  • AZD929/Osimertinib
  • Osimertinib Intermediate 4
  • Osimertinib, 98%, a potent and selective mutated forms EGFR inhibitor
  • Pharmaceutical Chemical Anticancer Drug Azd-9291 for for Lung Cancer 1421373-65-0
  • Mereletinib
  • N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide
  • Mereletinib mesylate(AZD9291)
CAS:
1421373-65-0
MF:
C28H33N7O2
MW:
499.61
EINECS:
629-848-5
Product Categories:
  • Inhibitors
  • API
  • AZD9291
  • Anticancer
  • 1421373-65-0
Mol File:
1421373-65-0.mol
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AZD-9291 Chemical Properties

Melting point:
>188oC (dec.)
Density 
1.19±0.1 g/cm3(Predicted)
storage temp. 
Hygroscopic, -20°C Freezer, Under inert atmosphere
solubility 
DMSO (Slightly, Heated), Methanol (Slightly, Heated)
pka
12.68±0.70(Predicted)
form 
Solid
color 
Pale Yellow to Beige
CAS DataBase Reference
1421373-65-0
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Safety Information

HS Code 
29339900
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AZD-9291 Usage And Synthesis

Uses

AZD-9291 (Osimertinib) is a oral, third generation, small-molecule epidermal growth factor receptor (EGFR) inhibitor and antineoplastic agent. In addition, it is a Cytochrome P450 3A inhibitor, and Cytochrome P450 3A4 Inducer, and Cytochrome P450 1A2 Inducer, and Breast Cancer Resistance Protein Inhibitor. It is used for the treatment of advanced non-small cell lung cancer (NSCLC) where mutant EGFR form (such as T790M) is often presented. Through suppressing the EGFR-mediated signalling, it cause cell death and inhibit tumour growth in related cancer cells. 

Description

AZD-9291 (Mesylate), also known as Osimertinib, belongs to a third-generation EGFR (epidermal growth factor receptor) inhibitor. It can be used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) in case when the cancer cells carry specific mutations (such as T790M) in the epidermal growth factor receptor. It takes effect through directly binding to the certain mutant forms of EGFR (T790M, L858R, and exon 19 deletions) that are frequently found in NSCLC, further causing poor prognosis for late-stage disease. Since it spares wild type EGFR during therapy, it has only limited toxicity.

Uses

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). AZD 9291 has been shown to inhibit tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients with advanced EGFR mutant non-small-cell lung cancer.[Cayman Chemical]

Definition

ChEBI: A member of the class of aminopyrimidines that is 4-(1-methylindol-3-yl)pyrimidin-2-amine in which one of the amino hydrogens is replaced by a 2-methoxy-4-[2-(dimethylamino)ethyl](methyl)amino-5-acrylamidophenyl group. Used (as the mesylate salt) for treat ent of EGFR T790M mutation positive non-small cell lung cancer.

Indications

The collection of ibrutinib (Imbruvica(R), Pharmacyclics Inc.), afatinib, and osimertinib represents the small, yet expanding, group of covalent SMKIs. Ibrutinib is a non-receptor Bruton’s tyrosine kinase inhibitor approved for the treatment of relapsed chronic lymphocytic leukemia. Afatinib, approved for NSCLC in 2013 and squamous NSCLC in 2016, is a second-generation irreversible EGFR inhibitor that targets wild-type EGFR, the mutant T790M EGFR, and HER2. Osimertinib (AZD9291), which was approved by FDA in November 2015, is a third-generation irreversible EGFR inhibitor that selectively targets the mutant T790M EGFR. Rociletinib, which shares a high degree of structural similarity with that of osimertinib, is a promising covalent EGFR inhibitor developed by Clovis Oncology aimed for the treatment of patients with EGFR T790M-mutated NSCLC, until the company terminated its development in May 2016 following a negative vote fromthe FDA’sOncologic Drugs Advisory Committee.

target

Exon 19 deletion EGFR

References

http://www.medkoo.com/products/6711
https://en.wikipedia.org/wiki/Osimertinib
https://www.drugbank.ca/drugs/DB09330

AZD-9291Supplier

Houxu Chemical (Shandong) Co., Ltd Gold
Tel
18295613325
Email
2026425403@qq.com
Absin Bioscience Inc. Gold
Tel
021-38015121 15000105423
Email
wulan@absin.cn
Shanghai Prescrina Pharmaceutical Technology Co., LTD Gold
Tel
18367323072
Email
2125193158@qq.com
Cangzhou Enke Pharma-tech Co., Ltd. Gold
Tel
0317-5296180 15533709196
Email
sale@enkepharma.com
TargetMol Chemicals Inc. Gold
Tel
021-021-33632979 15002134094
Email
marketing@targetmol.com