Osimertinib mesylate

ChemicalBook > CAS DataBase List > 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: 5mg
Price: $60
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FD146297
Product name: AZD 9291 mesylate
Packaging: 10mg
Price: $65
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

Tagrisso^TM

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

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:

ABT-199 THJ-018 Osimertinib dimesylate AZD-9291 Nintedanib Ethanesulfonate Salt GDC-0084 SH-4-54 Tazemetostat (EPZ-6438) Niraparib Mertansine (S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-triMethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate Enasidenib Ivosidenib ABBV-075 Ponatinib Selonsertib 2-(3-fluorophenyl)-3-methylmorpholine(3-fluorophenmetrazine)(3-FPM) ADB-FUBINACA

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)

Osimertinib

N-[2-(2-dimethylaminoethylmethylamino)-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide mesylate salt

Osimertinib Mesylate(AZD9291)

Osimertinib mesylate

Mereletinib mesylate

Mereletinib Ms salt

AZD9291 Ms salt, Osimertinib Ms salt

N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide methanesulfonate

Tagrisso

N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide methanesulfonate

AZD-9291 MESYLATE(OSIMERTINIB)

Osimertinib d6

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Osimertinib methanesulfonate

Osimertinib (AZD9291) mesylate

Mereletinib mesylate, 98%, a potent and selective mutated forms EGFR inhibitor

AZD-9291 (MESYLATE);TAGRISSO;OSIMERTINIB MESYLATE

AZD-9291 mesylate (Osimertinib mesylate

AZD-9291 mesylate (Osimertinib,Mereletinib)

MERELETINIB MESYLATE; EGFR INHIBITOR; AZD9291 MESYLATE; AZD 9291 MESYLATE;TAGRISSO

Mesylate-AZD9291

Osimertinib Mesylate (Tagrisso, Mereletinib, AZD-9291)

N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide methanesulfonate(AZD9291 mesylate)

Osimertinib Impurity 30

Mereletinib mesylateQ: What is Mereletinib mesylate Q: What is the CAS Number of Mereletinib mesylate Q: What is the storage condition of Mereletinib mesylate Q: What are the applications of Mereletinib mesylate

Undecanoicacid,15-hydroxy-

2-Propenamide, N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-, methanesulfonate (1:1)

Osimertinib mesylate (AZD-9291 mesylate)

N-2-2-(Dimethylamino)ethylmethylamino-4-methoxy-5-4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylaminophenyl-acrylamide methanesulfonate (1:1)

Osimertinib Mesylate API

Osimeitinib mesylate

osimertinib MsOH

PB1211

1421373-66-1

421373-66-1

C28H33N7O2CH4O3S

C29H37N7O5S

AZD09

API

1421373-66-1