An FGFR inhibitor
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Pemigatinib

Item No. 33260

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-1,3,4,7-tetrahydro-8-(4-morpholinylmethyl)-2H-pyrrolo[3′,2′:5,6]pyrido[4,3-d]pyrimidin-2-one
CAS Number
1513857-77-6
Synonyms
  • INCB054828
Molecular Formula
C24H27F2N5O4
Formula Weight
487.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMF:PBS (pH 7.2) (1:2): 0.33 mg/mlDMSO: 5 mg/ml
λmax
231, 289 nm
SMILES
O=C1N(CC2=CNC3=NC(CN4CCOCC4)=CC3=C2N1CC)C5=C(F)C(OC)=CC(OC)=C5F
InChi Code
InChI=1S/C24H27F2N5O4/c1-4-30-21-14(11-27-23-16(21)9-15(28-23)13-29-5-7-35-8-6-29)12-31(24(30)32)22-19(25)17(33-2)10-18(34-3)20(22)26/h9-11H,4-8,12-13H2,1-3H3,(H,27,28)
InChi Key
HCDMJFOHIXMBOV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $53

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    5 mg

    $218

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    10 mg

    $409

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    25 mg

    $825

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    Product Description

    Pemigatinib is an inhibitor of FGFR (IC50s = 0.4, 0.5, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).1 It is selective for FGFR1, FGFR2, and FGFR3 over FGFR4 and the kinase insert domain receptor (KDR; IC50s = 30 and 70 nM, respectively), as well as over a panel of 56 tyrosine and serine/threonine kinases at 10 µM. Pemigatinib reduces phosphorylation of FGFR, ERK1/2, and STAT5 in KG-1a acute myeloid leukemia cells in a concentration-dependent manner. It inhibits growth in a panel of cancer cell lines expressing constitutively active FGFR, including lung, bladder, and gastric cancer cells, with GI50 values ranging from 3 to 362 nM. Pemigatinib (0.3 mg/kg per day) reduces tumor growth in KATO III, KG-1, and RT-112 mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, P.C.C., Koblish, H., Wu, L., et al. INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models. PLoS One 15(4), e0231877 (2020).