Pemigatinib (INCB054828)

Catalog No.S0088 Synonyms: Pemazyre

For research use only.

Pemigatinib (INCB054828, Pemazyre) 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.

Pemigatinib (INCB054828) Chemical Structure

CAS No. 1513857-77-6

Selleck's Pemigatinib (INCB054828) has been cited by 4 Publications

Purity & Quality Control

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Biological Activity

Description Pemigatinib (INCB054828, Pemazyre) 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 Research:

[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 Research:

[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)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 487.50
Formula

C24H27F2N5O4

CAS No. 1513857-77-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN1C2=C3C=C(NC3=NC=C2CN(C1=O)C4=C(C(=CC(=C4F)OC)OC)F)CN5CCOCC5

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05216120 Not yet recruiting Drug: Pemigatinib 4.5 MG Pancreas Cancer HonorHealth Research Institute|Incyte Corporation August 2022 Phase 2
NCT03914794 Recruiting Drug: Pemigatinib Bladder Cancer|NMIBC|Non-Muscle Invasive Bladder Cancer|Urothelial Carcinoma Recurrent Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Incyte Corporation October 2 2020 Phase 2
NCT04258527 Completed Drug: Pemigatinib Solid Tumor Innovent Biologics (Suzhou) Co. Ltd. March 26 2020 Phase 1
NCT03235570 Completed Drug: Pemigatinib Solid Tumors Incyte Corporation August 1 2017 Phase 1
NCT02924376 Completed Drug: Pemigatinib Cholangiocarcinoma Incyte Corporation January 16 2017 Phase 2
NCT02872714 Completed Drug: pemigatinib UC (Urothelial Cancer) Incyte Corporation January 12 2017 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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