Home > Offer to Sell > Pharmaceuticals and Biochemicals > Hormones and synthetic substitutes > AZD-9291 (Mesylate)
AZD-9291 (Mesylate)
Inquiry
| Post Date: | Dec 23,2015 |
| Expiry Date: | Jun 20,2016 |
| Detailed Description: |
Cas No. :1421373-66-1
Quantity: 1000Kilograms Specs:99% Price:1 USD Kilograms Payment Method: T/T,MG,WU,BTC AZD-9291 (Mesylate) Synonyms:AZD-9291 (Mesylate);N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide methanesulfonate (1:1);AZD-9291 mesylate N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide methanesulfonate (1:1) CAS:1421373-66-1 MF:C28H33N7O2.CH4O3S AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM). IC50 value: 12.92 nM(Exon 19 deletion EGFR); 11.44 nM(L858R/T790M EGFR) [1] Target: L858R/T790M EGFR; Exon 19 deletion EGFR First-generation EGFR tyrosine kinase inhibitors (EGFR TKI) provide significant clinical benefit in patients with advanced EGFR-mutant (EGFRm) non-small cell lung cancer (NSCLC). Patients ultimately develop disease progression, usually due to the acquisition of the resistance mutation. AZD9291 is a oral, potent, and selective third generation irreversible inhibitor of both EGFRm sensitizing and T790M resistance mutants which spares wild-type EGFR. In vitro: AZD9291 potently inhibits signaling pathways and cellular growth in both EGFRm and EGFRm/T790M mutant cell lines, with lower activity against WT EGFR cell lines. AZD9291 showed an apparent IC50 of 12 nmol/L against L858R and 1 nmol/L against L858R/T790M EGFRm. In vivo: AZD9291 demonstrates good bioavailability, is widely distributed in tissues, and has moderate clearance resulting in a half-life of around 3 hours after oral dosing in the mouse . Once-daily dosing of AZD9291 induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models. The tumor shrinkage was observed at doses low to 2.5 mg kg-1 day-1 in both models. Clinical trial: The mesylate salt of AZD9291 is currently in a first-in-human phase I dose-escalation clinical trial (AURA; NCT01802632; AstraZeneca) in patients with advanced EGFRm NSCLC who had disease progression following treatment with any EGFR TKI (including gefitinib or erlotinib). AZD9291 is showing promising responses in this phase I trial even at the first-dose level. |
| CAS Registry Number: | 1421373-66-1 |
| Synonyms: | ;Osimertinib mesylate;N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide methanesulfonate (1:1);Osimertinib Mesylate;AZD-9291 mesylate; |
| Molecular Formula: | C28H33N7O2.CH4O3S |
| Molecular Weight: | 595.71 |
| Molecular Structure: | 
|
| Company: | Zhuhaishi Shuangbojie Technology Co.,Ltd. [ China ] |
| Contact: | Merry |
| Tel: | 18578209868 |
| Fax: | 0756-8889806 |
| Email: | mxy02@ycphar.com |
-
Disclaimer statement:The information and data included above have been realized by the enterprises and compiled by the staff, and are subject to change without notice to you. The Chemnet makes no warranties or representations whatsoever regarding the facticity, accuracy and validity of such information and data. In order to ensure your interest, we suggest you chose the products posted by our gold suppliers or VIP members.
