We supply AZD-9291 mesylate

We give AZD-9291 mesylate, a potent and largely picky third- generation epidermal growth factor receptor( EGFR) asset. AZD-9291 is used for the treatment ofnon-small cell lung cancer( NSCLC) with cranking EGFR mutations and resistance to first- line EGFR impediments. It's formulated as a white to out-white greasepaint and can be administered orally. Our AZD 9291 meets all the necessary quality norms and is available in colorful amounts to acclimatize to your specific exploration requirements. communicate us to learn further about our product or to place an order.

What's AZD-9291 mesylate?

AZD-9291 mesylate, also known as Osimertinib mesylate, is suitable for the treatment of adult cases with locally advanced or metastaticnon-small cell lung cancer( NSCLC) who have endured complaint progression during or after former treatment with epidermal growth factor receptor( EGFR) tyrosine kinase impediments( TKIs) and have been verified to have positive EGFRT790M mutations. AZD9291( methanesulfonic acid swab) has high selectivity, with an IC50 of11.4 nM and12.9 nM for T790M/ L858R mutations and exon 19 elisions of EGFR, independently, while its inhibitory exertion( IC50) for wild- type EGFR is 494nM. Osetinib is an unrecoverable asset of EGFR, which can form covalent bonds with molecular targets, so theoretically, the response lasts longer and the chance of developing resistance is similarly reduced.

Basic Information

Product Name: AZD-9291 mesylate

CAS:1421373-66-1

MF:C29H37N7O5S

MW:595.72

EINECS:200-064-1

MDL No.:MFCD28137994

Structural formula:

Purity: 99%+

Origin: China

Application: Anti-cancer

Delivery Time: stock

Melting point:>232 ° C (dec.)

Solubility: soluble in DMSO (a small amount) and methanol (a small amount)

Technical Specification:

Package: 10g;100g; 500g; 1kg

Storage conditions: -20 ° C Freezer, Under inner atmosphere

What is the Pharmacological action of AZD-9291 mesylate?

AZD-9291 mesylate is a targeted small-molecule inhibitor that selectively targets mutant epidermal growth factor receptor (EGFR) in non-small cell lung cancer (NSCLC) patients who have developed resistance to first and second generation EGFR inhibitors. The mesylate salt of AZD-9291 is a potent, irreversible inhibitor that has demonstrated excellent selectivity for mutant EGFR over wild-type EGFR in preclinical studies.

The pharmacological action of AZD9291 is to bind covalently and irreversibly to the cysteine residue of the EGFR kinase domain, leading to inhibition of kinase activity and subsequent suppression of downstream signaling pathways such as PI3K/Akt and MAPK/Erk1/2. This results in reduced tumor cell proliferation, survival, and migration, and ultimately leads to tumor regression.

In clinical studies, it has demonstrated significant efficacy in NSCLC patients harboring the EGFR T790M mutation, which is the most common mechanism of resistance to first and second generation EGFR inhibitors. In a phase I study, it showed a response rate of 51% in T790M-positive patients, with a higher response rate observed in patients who had received prior EGFR inhibitors. In a phase II study, it demonstrated a response rate of 60%, with a median progression-free survival of 9.6 months.

It has also been shown to have a favorable toxicity profile in clinical studies, with the most common adverse events being mild to moderate in severity and manageable with dose adjustments or supportive care. These common adverse events include diarrhea, rash, and nausea.

In conclusion, Osimertinib mesylate is a potent and highly selective inhibitor of mutant EGFR signaling that has demonstrated significant efficacy and a favorable toxicity profile in NSCLC patients harboring the EGFR T790M mutation. It represents a promising therapeutic option for patients with resistant NSCLC.

What is the application of AZD-9291 mesylate?

AZD-9291 mesylate is a highly potent and selective third-generation EGFR tyrosine kinase inhibitor (TKI) developed for the treatment of non-small cell lung cancer (NSCLC) patients with activating EGFR mutations and resistance to first-line EGFR TKIs. It selectively targets mutant EGFR and inhibits its activity, thereby blocking downstream signaling pathways, cell proliferation, and tumor growth. It has shown promising antitumor activity in preclinical and clinical studies, with a favorable safety profile and good tolerability.

It has been approved by the FDA for the treatment of metastatic NSCLC patients with the T790M mutation, who have progressed on or after EGFR TKI therapy. It is available in a tablet formulation for oral administration. The recommended dose is 80 mg once daily until disease progression or unacceptable toxicity occurs.

AZD9291 is a breakthrough therapy for NSCLC patients with EGFR mutations and resistance to first-line EGFR TKIs. It provides a new treatment option for patients who have exhausted other available therapies and have limited treatment options. Its high potency, selectivity, and favorable safety profile make it a promising candidate for further clinical development and expansion to other cancer indications. Further research and development are needed to explore its full potential and optimize its use in clinical practice.

Reference materials

1.ASO2014: AstraZeneca's new drug AZD9291 is effective against drug-resistant lung cancer. Dingxiangyuan [citation date 2016-11-17]

2. The Most Complete Cancer Targeted Drugs in History (2016 Edition). Dingxiangyuan [Cited 2016-11-16]

3.AZD9291 AstraZeneca's new drug is effective against drug-resistant lung cancer. Zhonghua Net [citation date 2016-11-16]

Contact information

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