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Ruxolitinib(JAK1/JAK2 inhibitor)

产品价格: ¥2988.00

最小起订量:暂无 可售数量:999盒

发货时限:
暂无
所在地区:
中国浙江杭州市
有效期至:
长期有效
最后更新:
2021-05-30 01:30:16
浏览次数:
51

产品详情

品牌名称:
Gene Operation
货号: IJS1003-0005MG
保存条件: -20℃
CAS号: 941678-49-5
供应商: 上海伟进生物科技有限公司
数量: 10
英文名: Ruxolitinib
保质期: 2 years
规格: 5mg

Biological Activity

Ruxolitinib (INCB018424) is a potent, selective and orally bioavailable inhibitor of JAK1 and JAK2 with IC50 of 2.7 and 4.5 nM, respectively. It shows modest selectivity against Tyk2 (IC50, 19 nM) and marked selectivity against JAK3 (IC50, 322 nM) [1]. INCB018424 inhibits IL-6 signaling (IC50, 281 nM), and proliferation of JAK2V617F+ Ba/F3 cells (IC50, 126 nM) as well as HEL cells (IC50, 186 nM) with JAK2 mutation. INCB018424 preferentially suppresses erythroid progenitor colony formation from JAK2V617F+ PV patients (IC50, 67 nM) versus healthy donors (IC50, >400 nM). In a mouse model of JAK2V617F+ MPN, oral INCB018424 markedly reduces splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminates neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects. The preclinical results support its clinical evaluation as a promising oral agent for the treatment of myeloproliferative neoplasms (MPNs), including MF, PV, and ET [2-3]. INCB018424 appears safe and well-tolerated dose of 15 mg BID and demonstrates preliminary efficacy in the treatment of Rheumatoid arthritis (RA) [4].

 

Chemical Properties

 

Cas No.: 941678-49-5

M. Wt.: 306.37

Formula: C17H18N6

Purity: >99%

Synonym: INCB018424, INCB18424, NCB018424, NCB18424

Chemical Name: (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl] propanenitrile

Appearance: White to off-white solid 

Solubility: Soluble in DMSO (20 mg/mL) and ethanol (15 mg/mL with warming), sparingly soluble in water

StorageStore solid at -20 ºC for the stability of two years

 

Application Concentration (Just for reference) 

 

The appropriate working concentration of Ruxolitinib depends on cell types, cell culture properties and specific applications. It is recommended that researchers start with optimal experiments for first use.

温馨提示:不可用于临床治疗。

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