Home Angiogenesis FGFR inhibitor Pemigatinib For research use only.

Pemigatinib

Synonyms: INCB054828

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.

Pemigatinib Chemical Structure

Pemigatinib Chemical Structure

CAS: 1513857-77-6

Selleck's Pemigatinib has been cited by 11 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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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
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]
Cell Research 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)
In Vivo
In vivo

No effect of pemigatinib on the disease course is evident on acute EAE.[2]
Animal Research 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)
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05216120 Withdrawn Pancreas Cancer HonorHealth Research Institute|Incyte Corporation June 14 2022 Phase 2
NCT03914794 Recruiting 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 Solid Tumor Innovent Biologics (Suzhou) Co. Ltd. March 26 2020 Phase 1
NCT03235570 Completed Solid Tumors Incyte Corporation August 1 2017 Phase 1
NCT02924376 Completed Cholangiocarcinoma Incyte Corporation January 16 2017 Phase 2

Chemical lnformation & Solubility

Molecular Weight 487.50 Formula

C24H27F2N5O4
CAS No. 1513857-77-6 SDF --
Smiles CCN1C2=C3C=C(NC3=NC=C2CN(C1=O)C4=C(C(=CC(=C4F)OC)OC)F)CN5CCOCC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 40 mg/mL ( (82.05 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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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.

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