Pemigatinib

Catalog No.S0088 Batch:S008802

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Technical Data

Formula

C24H27F2N5O4
Molecular Weight 487.50 CAS No. 1513857-77-6
Solubility (25°C)* In vitro DMSO 40 mg/mL (82.05 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.0mg/ml 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
Targets
FGFR1 [1]
(Cell-free assay)		 FGFR2 [1]
(Cell-free assay)		 FGFR3 [1]
(Cell-free assay)		 FGFR4 [1]
(Cell-free assay)
0.4 nM 0.5 nM 1.2 nM 30 nM
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]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Primary mouse astrocytes

  • Concentrations

    10 μM

  • Incubation Time

    24 h

  • Method

    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)
Animal Study:

[2]
  • Animal Models

    Female C57Bl/6J mice of experimental autoimmune encephalomyelitis (EAE) model

  • Dosages

    2.5 mg/kg

  • Administration

    i.n.

    (Data sourced from selleck products)

Selleck's Pemigatinib has been cited by 13 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.