Pemigatinib

Pemigatinib

CAT N°: 33260
Price:

From 72.00 61.20

Pemigatinib is an inhibitor of FGFR (IC50s = 0.4, 0.5, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).{59851} 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.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 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
  • Correlated keywords
    • INCB 054828 Pemazyre ERK-1/2 STAT-5 KG1a KG1 RT112 KATOIII
  • Product Overview:
    Pemigatinib is an inhibitor of FGFR (IC50s = 0.4, 0.5, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).{59851} 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.

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