產(chǎn)品描述
等級：活性藥物成分（API）
化學(xué)名稱：(3R)-環(huán)戊基-3-[4-(7H-吡咯并[2,3-d]嘧啶-4-基)吡唑-1-基]丙烯酰胺磷酸鹽
分子式：C17H21N6O4P
分子量：404.360
規(guī)格：根據(jù)《中國藥典》/《美國藥典》/《歐洲藥典》制定的企業(yè)標(biāo)準(zhǔn)
外觀：粉末狀
總雜質(zhì)含量：不超過0.5%
純度：不低于99%
殘留溶劑：完全符合ICH Q3C標(biāo)準(zhǔn)。
致突變雜質(zhì)：完全符合ICH M8標(biāo)準(zhǔn)
亞硝胺評估：已提供
粒徑：可提供常規(guī)等級產(chǎn)品或根據(jù)客戶要求進(jìn)行研磨/篩分。
儲存：常溫
生產(chǎn)能力：商業(yè)用途
標(biāo)準(zhǔn)包裝：1公斤/袋，5公斤/袋，或根據(jù)客戶要求
產(chǎn)品用途
簡介：Ruxolitinib是一種有效的JAK1/2抑制劑，IC50分別為3.3nM/2.8nM，比JAK3選擇性高130倍。
體外研究：Ruxolitinib（INCB018424）有效且選擇性地抑制JAK2V617F介導(dǎo)的信號傳導(dǎo)和增殖。Ruxolitinib抑制HEL細(xì)胞的生長，EC50為186nM。Ruxolitinib顯著增加Ba/F3-EpoR-JAK2V617F細(xì)胞系統(tǒng)的凋亡，并抑制原發(fā)性MPN患者樣本中的造血祖細(xì)胞增殖。
體內(nèi)研究：Ruxolitinib 可降低接種JAK2V617F表達(dá)細(xì)胞的小鼠的腫瘤負(fù)荷，而不會引起貧血或淋巴細(xì)胞減少。
生物活性：RuxolitinibPhosphate(INCB018424,INC424)是Ruxolitinib的磷酸鹽形式。Ruxolitinib是第一個(gè)應(yīng)用于臨床的，有效的，選擇性JAK1/2抑制劑，在無細(xì)胞試驗(yàn)中IC50為3.3nM/2.8nM。作用于JAK1，JAK2與作用于JAK3相比，選擇性高130多倍。Ruxolitinib通過毒性線粒體自噬殺死腫瘤細(xì)胞。Ruxolitinib可誘導(dǎo)自噬并增強(qiáng)細(xì)胞凋亡。
聯(lián)系方式
四川青木制藥有限公司
四川省眉山市東坡區(qū)經(jīng)濟(jì)開發(fā)區(qū)東區(qū)順江大道南段55號
國際營銷部(International):
Email: sales@eastonpharma.cn
Tel: 028-87827187
國內(nèi)營銷部(Mainland)：
李經(jīng)理 13880480517
楊經(jīng)理 15982276454
Product Description
· Grade: Active Pharmaceutical Ingredient(API)
· Chemical Name: (3R)-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propionitrile phosphate
· Molecular Formula: C17H21N6O4P
· Molecular Weight:404.360
· Specification: Enterprise Standard established according to ChP/USP/EP
· Appearance: Powder
· Total impurities: not more than 0.5%
· Purity: not less than 99%
· Residual Solvents: fully comply with ICH Q3C
· Mutagenic impurities: fully comply with ICH M8
· Nitrosamine assessment: available
· Particle size: regular grade or milling/sieving according to customer’s requirement.
· Storage: Room temperature
· Production capacity: Commercial
· Standard Package: 1kg/bag, 5kg/bag, or according to the customer’s requirement
Applications
· Ruxolitinib phosphate is a phosphate salt obtained by the reaction of ruxolitinib with one equivalent of phosphoric acid.
· Ruxolitinib API, formerly known as INCB018424 or INC424, is an anticancer drug and a Janus kinase (JAK) inhibitor. It is a potent and selective inhibitor of JAK1 and JAK2, which are tyrosine kinases involved in cytokine signaling and hematopoiesis. Myeloproliferative neoplasms, such as myelofibrosis and polycythemia vera, are often characterized by aberrant activation of the JAK-STAT pathway, leading to abnormal blood cell counts and thrombotic complications. By inhibiting JAK1 and JAK2, ruxolitinib works to block the dysregulated cell signaling pathways and prevents abnormal blood cell proliferation. Due to a large number of patients with myeloproliferative neoplasms who have JAK2 mutations, ruxolitinib was the first ATP-competitive inhibitor of JAK1 and JAK2 ever developed.
· Ruxolitinib was first approved for the treatment of adult patients with myelofibrosis by the FDA in 2011, followed by EMA‘s approval in 2012. In 2014, it was approved for the treatment of polycythemia vera in adults who have an inadequate response to or are intolerant of hydroxyurea, and in 2019, ruxolitinib was approved for use in steroid-refractory acute graft-versus-host disease in adults, and children. The topical formulation of ruxolitinib is used to treat atopic dermatitis and vitiligo. It is being investigated for other inflammatory skin conditions.
· Ruxolitinib has been investigated to treat patients with coronavirus disease 2019 (COVID-19) accompanied by severe systemic hyperinflammation. In phase II clinical trials, ruxolitinib improved chest computed tomography and improved recovery in patients with lymphopenia. However, phase III clinical trials later determined that ruxolitinib was inadequate in meeting its primary endpoint of reducing the number of hospitalized COVID-19 patients who experienced severe complications thus the drug was not approved as a treatment for COVID-19.
Contact Information
Sichuan Qingmu Pharmaceutical Co., Ltd.
Add: No. 55, South Shunjiang Avenue, East Economic Development Zone, Dongpo District, Meishan City, Sichuan, 620036, China
International Marketing Department:
Email: sales@eastonpharma.cn
Tel: 0086-28-87827187