Pemigatinib

製品コードS0088 バッチS008802

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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.000mg/ml (4.10mM) Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 this compound 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 this compound 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)

参考

  • https://pubmed.ncbi.nlm.nih.gov/31770593/
  • https://pubmed.ncbi.nlm.nih.gov/35393953/

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：

PRIMARY CUTANEOUS CD8+ AGGRESSIVE EPIDERMOTROPIC CYTOTOXIC T-CELL LYMPHOMA WITH NOVEL FGFR1 FUSION TREATED WITH PEMIGATINIB [ Blood Adv, 2025, bloodadvances.2024014928.] PubMed: 39825823
Coordinated inheritance of extrachromosomal DNAs in cancer cells [ Nature, 2024, 635(8037):201-209] PubMed: 39506152
FGFR inhibition blocks NF-ĸB-dependent glucose metabolism and confers metabolic vulnerabilities in cholangiocarcinoma [ Nat Commun, 2024, 15(1):3805] PubMed: 38714664
Chromatin Remodeling in Patient-Derived Colorectal Cancer Models [ Adv Sci (Weinh), 2024, 11(16):e2303379] PubMed: 38380561
Sensitizing cholangiocarcinoma to chemotherapy by inhibition of the drug-export pump MRP3 [ Biomed Pharmacother, 2024, 180:117533] PubMed: 39405909
iPSC-derived megakaryocytes and platelets accelerate wound healing and angiogenesis [ Stem Cell Res Ther, 2024, 15(1):364] PubMed: 39402677
A highly efficient, scalable pipeline for fixed feature extraction from large-scale high-content imaging screens [ iScience, 2024, 27(12):111434] PubMed: 39720532
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
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

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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