An inhibitor of FGFR
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Derazantinib

Item No. 27636

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(6R)-6-(2-fluorophenyl)-5,6-dihydro-N-[3-[2-[(2-methoxyethyl)amino]ethyl]phenyl]-benzo[h]quinazolin-2-amine
CAS Number
1234356-69-4
Synonyms
  • ARQ 087
Molecular Formula
C29H29FN4O
Formula Weight
468.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:3): 0.25 mg/mlDMSO: 25 m/gml
λmax
248, 281, 353 nm
SMILES
COCCNCCC1=CC=CC(NC2=NC=C3C(C4=CC=CC=C4[C@H](C5=C(F)C=CC=C5)C3)=N2)=C1
InChi Code
InChI=1S/C29H29FN4O/c1-35-16-15-31-14-13-20-7-6-8-22(17-20)33-29-32-19-21-18-26(24-10-4-5-12-27(24)30)23-9-2-3-11-25(23)28(21)34-29/h2-12,17,19,26,31H,13-16,18H2,1H3,(H,32,33,34)/t26-/m1/s1
InChi Key
KPJDVVCDVBFRMU-AREMUKBSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Product Description

    Derazantinib is a multi-kinase inhibitor.1 It is a pan inhibitor of FGF receptors (FGFRs; IC50s = 4.5, 1.8, 4.5, and 34 nM for FGFR1, -2, -3, and -4, respectively) and also inhibits 10 receptor tyrosine kinases, 8 non-receptor tyrosine kinases, and the calcium/calmodulin-dependent protein kinase QIK in a panel of 297 kinases (IC50s = 3-31 and 9.7 nM, respectively). Derazantinib decreases phosphorylation of FGFR in COS-1 cells expressing FGFR1, -2, -3, or -4 (IC50s = <0.123, 0.185, 0.463, and >10 µM, respectively) and inhibits the growth of 15 cancer cell lines with mutant, amplified, or translocated FGFR (GI50s = 0.1-1.7 µM). It reduces tumor growth and decreases tumor protein levels of phosphorylated FGFR, FGFR substrate 2 (FRS2), and ERK in a SNU-16 mouse xenograft model when administered at doses of 50 and 75 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hall, T.G., Yu, Y., Eathiraj, S., et al. Preclinical activity of ARQ 087, a novel inhibitor targeting FGFR dysregulation. PLoS One 11(9), e0162594 (2016).