Olmutinib | China | Manufacturer | Shandong Huisheng Import & Export Co., Ltd.

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Product Details

Product Name: Olmutinib	CAS No.: 1353550-13-6
Min. Order: 1KG	Purity: 98%~99%
Supply Ability: 20 T each week	Release date: 2023/08/13

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Product Name:	Olmutinib
Synonyms:	HM71224;HM-71224;Olmutinib;Olmutinib, HM71224;N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide dihydrochloride monohydrate;N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide;N-[3-[[2-[[4-(4-Methyl-1-piperazinyl)phenyl]amino]thieno[3,2-d]pyrimidin-4-yl]oxy]phenyl]-2-propenamide;HM71224, Olmutinib
CAS:	1353550-13-6
MF:	C26H26N6O2S
MW:	486.59
EINECS:
Product Categories:
Mol File:	1353550-13-6.mol

Olmutinib Chemical Properties

density	1.336±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	insoluble in H2O; ≥9.11 mg/mL in EtOH with ultrasonic; ≥96.6 mg/mL in DMSO
form	crystalline solid
pka	12.87±0.70(Predicted)

Olmutinib Usage And Synthesis

Description	Olmutinib, codeveloped by Boehringer Ingelheim and Hanmi Pharmaceutical Co., was approved by the Korean Ministry of Food and Drug Safety (MFDS) for treatment of locally advanced or metastatic EGFR T790 M mutation-positive non-small cell lung cancer (NSCLC). Olmutinib serves as a third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI), which is being used as an oral therapy for patients who have previously been treated with an alternate EGFR TKI. Firstand second-generation EGFR TKIs, which bind reversibly and irreversibly to the TK domain, respectively, are both generally effective at onset of treatment but result in development of resistance within the first year of treatment. Thirdgeneration EGFR TKIs such as olmutinib have demonstrated the ability to covalently bind to the kinase domain of EGFR while sparing wild-type EGFR, leading to irreversible inhibition of both EGFR mutations and the T790 M mutation, which is linked to EGFR TKI resistance.
Description	HM61713 is a third generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that inhibits both EGFR activating and T790M resistance mutations, while sparing wild-type EGFR. It has been investigated in Phase II clinical trials in patients with EGFR T790M mutation-positive non-small cell lung cancer (NSCLC), who developed resistance to earlier generations of EGFR tyrosine kinase inhibitor therapy.
Uses	Olmutinib is an epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) against non-small cell lung cancer (NSCLC).
Synthesis	Synthetically, olmutinib can be accessed in two steps beginning with 2,4-dichloro-thieno[3,2-d]pyrimidine (147), which is commercially available and can be prepared in two steps from urea and 3-aminothiophene 2- carboxylate. Nucleophilic addition of N-(3-hydroxyphenyl)-2- propenamide (148) to 147 proceeded with complete regioselectivity via treatment with K2CO3 in warm DMSO, smoothly providing the desired diaryl ether 149 in 87% yield after crystallization from isopropanol and water. From 149, substitution with commercially available piperazinyl aniline 150 under acidic heating conditions (DMA, IPA, TFA, 90 ??C) provided olmutinib in 82% yield. After recrystallization, olmutinib (XVI) was obtained in 60% overall yield and 99.1% purity.
in vitro	olmutinib has been identified as an irreversible kinase inhibitor and could covalently bind to a cysteine residue near the kinase domain of mutant egfr. olmutinib had a half-life of over 24h for egfr inhibition. olmutinib was able to cause potent inhibition in cell lines h1975 (l858r and t790m) and hcc827 (exon 19 deletion). olmutinib showed a low potency for nsclc cell line h358 with wild-type egfr [1].
in vivo	the previous in vivo studies of xenograft models with grafts of h1975 and hcc827 showed that olmutinib was active against the tumors without dasplaying any side effects [1].
references	[1] wang s, cang s, liu d. third-generation inhibitors targeting egfr t790m mutation in advanced non-small cell lung cancer. j hematol oncol. 2016 apr 12;9:34.

Olmutinib Preparation Products And Raw materials

Raw materials

2-Chlorothieno[3,2-d]pyriMidin-4(3H)-one-->2,4-Dichlorothieno[3,2-d]pyrimidine-->N-(3-hydroxyphenyl)acrylamide-->2-Mercaptothieno[3,2-d]pyrimidin-4(1H)one-->2-(Methylsulfanyl)thieno[3,2-d]pyrimidin-4(1H)one-->4-(4-Methylpiperazino)aniline-->Acryloyl chloride

Company Profile Introduction

Shandong Huisheng Import & Export Co., Ltd. is located in Jinan city, Shandong Province, is a collection of domestic trade, international trade in one of the diversified services company. Our goal is to provide customers with high quality solutions and one-stop purchasing experience. At present, the company business scope involves five areas: Organic chemical raw materials, inorganic chemical raw materials, fine chemical raw materials, dangerous chemicals and green environmental protection chemical technology project promotion, and we has also established good relations of cooperation with several well-known enterprises and won the strong support of extensive trust from the new and old customers. Products are widely used in automobile, household appliances, office supplies, mobile phone accessories, routers, food, medical and other fields. At present, our business covers 30 countries, and our customers mainly come from Australia, New Zealand, Canada, Germany, France, Poland, South Korea, Russia, Bangladesh, Vietnam, Kazakhstan, India, Ghana, Nigeria, South Africa, Egypt and other more than 30 countries. The company has a sound quality management system and advanced professional equipment, with a positive attitude to meet the changing needs of customers. We take "quality products, quality service, competitive price, timely delivery" as the purpose, looking forward to greater cooperation with overseas customers on the basis of mutual benefit. Our company provides a wide range of products to meet your various needs. Since its inception, the company has always adhered to the "quality first, customer first, reputation first" business policy, wholeheartedly meet the potential needs of our customers. Under the irresistible situation of economic globalization, our company is willing to cooperate sincerely with enterprises around the world to achieve a win-win situation.

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Shandong Huisheng Import & Export Co., Ltd.

Min. Order:	1KG
Supply Ability:	20 T each week
Update Time:	2023-08-13