Osimertinib mesylate
- Product Name
- Osimertinib mesylate
- CAS No.
- 1421373-66-1
- Chemical Name
- Osimertinib mesylate
- Synonyms
- Osimertinib;Tagrisso;Osimertinib d6;Mereletinib mesylate;Osimertinib methanesulfonate;Osimertinib (AZD9291) mesylate;N-[2-(2-dimethylaminoethylmethylamino)-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide mesylate salt;N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide methanesulfonate;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);PB1211
- CBNumber
- CB82677060
- Molecular Formula
- C29H37N7O5S
- Formula Weight
- 595.72
- MOL File
- 1421373-66-1.mol
Osimertinib mesylate Property
- Melting point:
- >232°C (dec.)
- storage temp.
- -20°C Freezer, Under inert atmosphere
- solubility
- DMSO (Slightly), Methanol (Slightly)
- form
- Solid
- color
- Off-White to Yellow
- InChI
- InChI=1S/C28H33N7O2.CH4O3S/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;1-5(2,3)4/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32);1H3,(H,2,3,4)
- InChIKey
- FUKSNUHSJBTCFJ-UHFFFAOYSA-N
- SMILES
- S(O)(=O)(=O)C.CN1C2=CC=CC=C2C(C2C=CN=C(NC3C=C(NC(=O)C=C)C(N(C)CCN(C)C)=CC=3OC)N=2)=C1
Safety
- HS Code
- 29339900
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H302Harmful if swallowed
H317May cause an allergic skin reaction
H361Suspected of damaging fertility or the unborn child
H372Causes damage to organs through prolonged or repeated exposure
H400Very toxic to aquatic life
H410Very toxic to aquatic life with long lasting effects
- Precautionary statements
-
P201Obtain special instructions before use.
P202Do not handle until all safety precautions have been read and understood.
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P272Contaminated work clothing should not be allowed out of the workplace.
P273Avoid release to the environment.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P281Use personal protective equipment as required.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P308+P313IF exposed or concerned: Get medical advice/attention.
P314Get medical advice/attention if you feel unwell.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P333+P313IF SKIN irritation or rash occurs: Get medical advice/attention.
P363Wash contaminated clothing before reuse.
P391Collect spillage. Hazardous to the aquatic environment
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- A808205
- Product name
- AZD-9291Mesylate
- Packaging
- 25mg
- Price
- $45
- Updated
- 2021/12/16
- Product number
- A808205
- Product name
- AZD-9291Mesylate
- Packaging
- 100mg
- Price
- $60
- Updated
- 2021/12/16
- Product number
- 474070
- Product name
- AZD 9291 mesylate
- Packaging
- 100mg
- Price
- $1168
- Updated
- 2021/12/16
- Product number
- CS-2019
- Product name
- Osimertinibmesylate
- Purity
- 99.94%
- Packaging
- 1g
- Price
- $190
- Updated
- 2021/12/16
- Product number
- CS-0131988
- Product name
- OsimertinibD6
- Purity
- 99.70%
- Packaging
- 1mg
- Price
- $420
- Updated
- 2021/12/16
Osimertinib mesylate Chemical Properties,Usage,Production
Description
Osimertinib is active against exon 19 deletions, exon 21 mutations, and also the exon 20 T790M mutations. It is preferentially selective for mutated EGFR, and therefore toxicity at therapeutic doses is lower than for first- and second-generation agents. Notably, osimertinib is able to cross the blood-brain barrier, making it active against disease in the CNS.
Uses
Osimertinib mesylate (AZD9291) is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug.
Application
Osimertinib mesylate is approved to treat: Non-small cell lung cancer that has certain EGFR gene mutations. It is used in adults: As adjuvant therapy after surgery to remove the cancer; As the first therapy for cancer that has spread to other parts of the body, or in patients whose cancer has spread to other parts of the body and got worse during or after treatment with another EGFR tyrosine kinase inhibitor.
Definition
ChEBI: A methanesulfonate (mesylate) salt prepared from equimolar amounts of osimertinib and methanesulfonic acid. Used for treatment 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.
brand name
TagrissoTM
General Description
Class: receptor tyrosine kinase
Treatment: NSCLC
Oral bioavailability = 70%
Elimination half-life = 48 h
Protein binding = 94.7%
Side effects
Osimertinib toxicity is dose-dependent and is associated with fewer gastrointestinal and dermatologic adverse events than with other approved EGFR TKIs.
Synthesis
Friedel-Crafts arylation of commercial N-methylindole
(203) with commercial dichloropyrimidine 202 gave the 3-
pyrazinyl indole 204 in good yield. Subsequent SNAr with
nitroaniline 205 (available from a one-step nitration from the
commercially available des-nitroaniline) provided aminopyrazine
206. Next, SN
Ar reaction of 206 with N,N,N??-
trimethylated ethylenediamine delivered 207 in near quantitative
yield, and this was followed by nitro reduction with iron
under acidic conditions to give rise to the triaminated arene
208 in 85% yield. Because acrylates are notoriously difficult to
install directly due to their highly reactive nature and
propensity to polymerize, a clever two-step acylation/
elimination sequence was employed using 3-chloropropanoyl
chloride, and this was immediately followed by mesylate salt
formation, which furnished the osimertinib mesylate (XXVI) in
excellent yield. This seven-step process which derives from
readily available feedstock delivered the final product in nearly
57% overall yield from starting materials 202 and 203.
Osimertinib mesylate Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Osimertinib mesylate manufacturers
- Product
- Osimertinib mesylate 1421373-66-1
- Price
- US $0.00-0.00/kg
- Min. Order
- 1kg
- Purity
- ＞99.5% by HPLC
- Supply Ability
- 100kg/month
- Release date
- 2023-02-18
- Product
- Osimertinib mesylate 1421373-66-1
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99
- Supply Ability
- 1
- Release date
- 2024-09-20
- Product
- Osimertinib mesylate 1421373-66-1
- Price
- US $0.00/Kg/Bag
- Min. Order
- 100g
- Purity
- 99.5%min
- Supply Ability
- 10kg
- Release date
- 2021-08-19