Pemigatinib (Synonyms: INCB054828)
目录号: PL01751 纯度: ≥99%
CAS No. :1513857-77-6
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中文名称
Pemigatinib
英文名称
Pemigatinib
英文别名
Pemigatinib;INCB054828;Y6BX7BL23K;3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one;3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-[(morpholin-4-yl)methyl]-1,3,4,7-tetrahydro-2Hpyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2-one;Pemazyre;Pemazyre (TN);Pemigatinib [INN];Pemigatinib [USAN];Pemigatinib [USAN:INN];Fgfr inhibitor INCB054828;Pemigatinib (JAN/USAN/INN);GTPL9767;Pemig
Cas No.
1513857-77-6
分子式
C24H27F2N5O4
分子量
487.50
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Pemigatinib (INCB054828) 是一种具有口服活性的,选择性 FGFR 抑制剂,对于 FGFR1,FGFR2,FGFR3,FGFR4 的 IC50 分别为 0.4 nM,0.5 nM,1.2 nM,30 nM。Pemigatinib 有用于胆管癌的潜力。
生物活性
Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC 50 s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.
性状
Solid
IC50 & Target[1][2]
FGFR1 0.4 nM (IC50) FGFR2 0.5 nM (IC5
体外研究(In Vitro)
This hypothesis is corroborated with in vitro cell-based studies in which cells expressing FGFR2-CLIP1 fusion are sensitive to Pemigatinib (INCB054828; IC50 value of 10.16 nM), whereas cells with the addition of the N549H mutation are resistant to Pemigatinib (IC50 value of 1527.57 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Arudra K, et al. Calcinosis cutis dermatologic toxicity associated with fibroblast growth factor receptor inhibitor for the treatment of Wilms tumor. J Cutan Pathol. 2018 Oct;45(10):786-790.
[2]. Roskoski R Jr, et al. The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder. Pharmacol Res. 2020 Jan;151:104567.
溶解度数据
In Vitro: DMSO : 25 mg/mL (51.28 mM; ultrasonic and warming and heat to 60°C)配制储备液
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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