Pemigatinib

製品コードS0088 バッチS008801

印刷

化学情報

Chemical Structure Synonyms INCB054828 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C24H27F2N5O4
分子量 487.50 CAS No. 1513857-77-6
Solubility (25°C)* 体外 DMSO 40 mg/mL (82.05 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Pemigatinib is an orally active and selective inhibitor of FGFR with IC50 of 0.4 nM, 0.5 nM, 1.2 nM and 30 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.
in vitro

Pemigatinib successfully diminishes the capacity of reactive astrocytes to recruit myeloid cells. Potentially FGFR modulation by pemigatinib may be promising for suppression of proinflammatory astrocyte responses while, at the same time, promoting protective mechanisms in murine and human systems.[2]
in vivo

No effect of pemigatinib on the disease course is evident on acute EAE.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Primary mouse astrocytes
濃度 10 μM
反応時間 24 h
実験の流れ

Primary mouse astrocytes were stimulated with afatinib (10 μM), UNC2025 (10 μM), or pemigatinib (10 μM) for 24 hours. N2A neuronal cells were stimulated with ACM or control medium for 24 hours. Primary mouse astrocytes and N2A neuronal cells were detached and washed once in cold 1× PBS. Live/dead staining was performed. In addition, annexin V–propidium iodide staining was performed. Cells were washed once and resuspended in annexin V binding buffer before acquisition on a 3L Cytek Northern Lights flow cytometer. Analysis of flow cytometry data was performed with the OMIQ platform.

(Data sourced from selleck products)
動物実験 動物モデル Female C57Bl/6J mice of experimental autoimmune encephalomyelitis (EAE) model
投薬量 2.5 mg/kg
投与方法 i.n.

(Data sourced from selleck products)

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] PubMed: 37377403
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] PubMed: 37377403
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] PubMed: 37377403
A DNA/RNA heteroduplex oligonucleotide coupling asparagine depletion restricts FGFR2 fusion-driven intrahepatic cholangiocarcinoma [ Mol Ther Nucleic Acids, 2023, 34:102047] PubMed: 37869260
Distinct mechanisms for sebaceous gland self-renewal and regeneration provide durability in response to injury [ Cell Rep, 2023, 42(9):113121] PubMed: 37715952
Coordinated inheritance of extrachromosomal DNA species in human cancer cells [ bioRxiv, 2023, 2023.07.18.549597] PubMed: 37503111
Distinct mechanisms for sebaceous gland self-renewal and regeneration provide durability in response to injury [ bioRxiv, 2023, 2023.05.05.539454] PubMed: 37205445
EGFR Inhibition Potentiates FGFR Inhibitor Therapy and Overcomes Resistance in FGFR2 Fusion-Positive Cholangiocarcinoma [ Cancer Discov, 2022, 12(5):1378-1395] PubMed: 35420673
Intranasal delivery of a small-molecule ErbB inhibitor promotes recovery from acute and late-stage CNS inflammation [ JCI Insight, 2022, 7(7)e154824] PubMed: 35393953
Carcinoma of unknown primary: Molecular tumor board-based therapy [ CA Cancer J Clin, 2022, 2(6):510-523.] PubMed: 36006378

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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