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Pemigatinib

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Chemical Structure| 1513857-77-6 同义名 : INCB054828
CAS号 : 1513857-77-6
货号 : A1176662
分子式 : C24H27F2N5O4
纯度 : 99%+
分子量 : 487.499
MDL号 : MFCD31706227
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(51.28 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • FGFR2

    FGFR2, IC50:0.5 nM

  • FGFR3

    FGFR3, IC50:1.2 nM

  • FGFR4

    FGFR4, IC50:30 nM

  • FGFR1

    FGFR1, IC50:0.4 nM
描述 Fibroblast growth factor receptor (FGFR) tyrosine kinases, which are expressed on the cell membrane, are involved in a wide range of biological functions such as cell proliferation, survival, migration, and differentiation. The identification of FGFR fusions and other alterations in a wide range of solid tumors, including cholangiocarcinoma and bladder cancer, has resulted in the development of several selective FGFR inhibitors for use in these indications, for example, infigratinib, erdafitinib, derazantinib, pemigatinib, and futibatinib[1]. Pemigatinib is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) types 1, 2, and 3, with potential antineoplastic activity[2]. It is used for the treatment of adults with previously treated, unresectable, locally advanced or metastatic cholangiocarcinoma and a FGFR2 fusion or other rearrangement (13.5mg once daily)[3]. Pemigatinib was investigated using xenograft tumor models with genetic alterations in FGFR1, 2, or 3. Enzymatic assays with recombinant human FGFR kinases showed potent inhibition of FGFR1, 2, and 3 by Pemigatinib (half maximal inhibitory concentration [IC50] 0.4, 0.5, and 1.0 nM, respectively) with weaker activity against FGFR4 (IC50 30 nM). Pemigatinib selectively inhibited growth of tumor cell lines with activation of FGFR signaling. The preclinical pharmacokinetic profile suggests target inhibition is achievable by Pemigatinib in vivo with low oral doses and the combination of Pemigatinib with cisplatin provided significant benefit over either single agent, with an acceptable tolerability[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.21mL

10.26mL

2.05mL

1.03mL

20.51mL

4.10mL

2.05mL
参考文献

[1]Mario E Lacouture,et al. Dermatologic Adverse Events Associated with Selective Fibroblast Growth Factor Receptor Inhibitors: Overview, Prevention, and Management Guidelines. Oncologist. 2021. 26(2), e316-e326.

[2]National Center for Biotechnology Information (2022). PubChem Compound Summary for CID 86705695, Pemigatinib. Retrieved September 27, 2022.

[3]Hoy, S. M. Pemigatinib: First Approval. Drugs. 2020. 80, 923-929.

[4]Liu, P. C. C., Koblish, H. et al. INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models. PLOS ONE. 2020.