A pan-FGFR inhibitor
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JNJ-42756493

Item No. 21813

Technical Information
Formal Name
N1-(3,5-dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine
CAS Number
1346242-81-6
Synonyms
  • Erdafitinib
Molecular Formula
C25H30N6O2
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:7): 0.12 mg/mlDMSO: 10 mg/mlEthanol: 1 mg/ml
λmax
224, 257, 297, 411 nm
SMILES
COC1=CC(OC)=CC(N(CCNC(C)C)C2=CC=C(N=CC(C3=CN(C)N=C3)=N4)C4=C2)=C1
InChi Code
InChI=1S/C25H30N6O2/c1-17(2)26-8-9-31(20-10-21(32-4)13-22(11-20)33-5)19-6-7-23-24(12-19)29-25(15-27-23)18-14-28-30(3)16-18/h6-7,10-17,26H,8-9H2,1-5H3
InChi Key
OLAHOMJCDNXHFI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    JNJ-42756493 is a pan-FGFR inhibitor (IC50s = 1.2, 2.5, 3, and 5.7 nM for FGFR1, -2, -3, and -4, respectively).1 It is selective for FGFRs over VEGFR2 (IC50 = 36.8 nM). JNJ-42756493 inhibits the proliferation of Ba/F3 cells expressing FGFR1, -3, or -4 (IC50s = 22.1, 13.2, and 25 nM, respectively). It reduces tumor growth in a SNU-16 gastric cancer mouse xenograft model when administered at doses of 10 and 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Perera, T.P.S., Jovcheva, E., Mevellec, L., et alDiscovery and pharmacological characterization of JNJ-42756493 (erdafitinib), a functionally selective small molecule FGFR family inhibitor. Mol. Cancer Ther. 16(6), 1010-1020 (2017).