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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
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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
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Safety

HS Code 
29339900
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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..…

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N-Bromosuccinimide Price

TRC
Product number
A808205
Product name
AZD-9291Mesylate
Packaging
25mg
Price
$45
Updated
2021/12/16
TRC
Product number
A808205
Product name
AZD-9291Mesylate
Packaging
100mg
Price
$60
Updated
2021/12/16
Usbiological
Product number
474070
Product name
AZD 9291 mesylate
Packaging
100mg
Price
$1168
Updated
2021/12/16
ChemScene
Product number
CS-2019
Product name
Osimertinibmesylate
Purity
99.94%
Packaging
1g
Price
$190
Updated
2021/12/16
ChemScene
Product number
CS-0131988
Product name
OsimertinibD6
Purity
99.70%
Packaging
1mg
Price
$420
Updated
2021/12/16
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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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Osimertinib mesylate Suppliers

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View Lastest Price from Osimertinib mesylate manufacturers

Zison Pharmaceutical (Shandong) Co., Ltd.
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
S&Y Biochem Co.,Ltd
Product
Osimertinib mesylate 1421373-66-1
Price
US $1.00/g
Min. Order
1g
Purity
99
Supply Ability
1
Release date
2024-09-20
WUHAN FORTUNA CHEMICAL CO., LTD
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

1421373-66-1, Osimertinib mesylateRelated Search:


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