磷酸芦可替尼;磷酸鲁索替尼；1092939-17-7；Ruxolitinib Phosphate 新品

产品描述

Ÿ   等级：活性药物成分（API）

Ÿ   化学名称：(3R)-环戊基-3-[4-(7H-吡咯并[2,3-d]嘧啶-4-基)吡唑-1-基]丙烯酰胺磷酸盐

Ÿ   分子式：C17H21N6O4P

Ÿ   分子量：404.360

Ÿ   规格：根据《中国药典》/《美国药典》/《欧洲药典》制定的企业标准

Ÿ   外观：粉末状

Ÿ   总杂质含量：不超过0.5%

Ÿ   纯度：不低于99%

Ÿ   残留溶剂：完全符合ICH Q3C标准。

Ÿ   致突变杂质：完全符合ICH M8标准

Ÿ   亚硝胺评估：已提供

Ÿ   粒径：可提供常规等级产品或根据客户要求进行研磨/筛分。

Ÿ   储存：常温

Ÿ   生产能力：商业用途

Ÿ   标准包装：1公斤/袋，5公斤/袋，或根据客户要求

产品用途

Ÿ   简介：Ruxolitinib是一种有效的JAK1/2抑制剂，IC50分别为3.3nM/2.8nM，比JAK3选择性高130倍。

Ÿ   体外研究：Ruxolitinib（INCB018424）有效且选择性地抑制JAK2V617F介导的信号传导和增殖。Ruxolitinib抑制HEL细胞的生长，EC50为186nM。Ruxolitinib显着增加Ba/F3-EpoR-JAK2V617F细胞系统的凋亡，并抑制原发性MPN患者样本中的造血祖细胞增殖。

Ÿ   体内研究：Ruxolitinib 可降低接种JAK2V617F表达细胞的小鼠的肿瘤负荷，而不会引起贫血或淋巴细胞减少。

Ÿ   生物活性：RuxolitinibPhosphate(INCB018424,INC424)是Ruxolitinib的磷酸盐形式。Ruxolitinib是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3nM/2.8nM。作用于JAK1，JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib可诱导自噬并增强细胞凋亡。

联系方式

四川青木制药有限公司

四川省眉山市东坡区经济开发区东区顺江大道南段55号

国际营销部(International):

Email: sales@eastonpharma.cn 

Tel: 028-87827187

国内营销部(Mainland)：

李经理 13880480517   

杨经理 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