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CAS No.: 1513857-77-6

Pemigatinib/培米加替尼 Catalog No. CSN26440

Synonyms: INCB054828

Pemigatinib, also known as INCB054828, is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) types 1, 2, and 3 (FGFR1/2/3), with potential antineoplastic activity. FGFR inhibitor INCB054828 binds to and inhibits FGFR1/2/3, which may result in the inhibition of FGFR1/2/3-related signal transduction pathways. This inhibits proliferation in FGFR1/2/3-overexpressing tumor cells.

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技术信息

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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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0513 mL
- 10.2564 mL
- 20.5129 mL
- 5 mM
- 0.4103 mL
- 2.0513 mL
- 4.1026 mL
- 10 mM
- 0.2051 mL
- 1.0256 mL
- 2.0513 mL

技术信息

CAS号

1513857-77-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H27F2N5O4

运输

蓝冰

分子量

487.50

别名

INCB054828

溶解度

DMSO	40.0 mg/mL (82.1 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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