1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. E7090 succinate

E7090 succinate 

Cat. No.: HY-101466A
Handling Instructions

E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively.

For research use only. We do not sell to patients.

E7090 succinate Chemical Structure

E7090 succinate Chemical Structure

CAS No. : 1879965-80-6

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Description

E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively[1].

IC50 & Target[2]

FGFR1

0.71 nM (IC50)

FGFR2

0.50 nM (IC50)

FGFR3

1.2 nM (IC50)

FGFR4

120 nM (IC50)

In Vitro

E7090 also inhibited the growth of SNU-16, human gastric cancer cell line harboring FGFR2 amplification with an IC50 value of 3 nM[1].
E7090 succinate inhibited SNU-16 cell proliferation with an IC50 value of 5.7 nM[2].
E7090 inhibits proliferation of human cancer cell lines harboring various types of FGFRs gene abnormalities such as amplification, mutation, or translocation in vitro, which are confirmed by the inhibition of FGFR signaling[1].
E7090 succinate has interaction kinetics with FGFR1 kinases intermediate between those of the two representative inhibitors, and the residence time of E7090 succinate is 19 minutes[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: SNU-16 cells.
Concentration: 0.4-100 nM.
Incubation Time: 4 h.
Result: Inhibited FGFR phosphorylation with an IC50 value of 1.2 nmol/L. Inhibited the phosphorylation of FRS2a, ERK1/2, and AKT, molecules downstream of FGFRs, in a dose-dependent manner.
In Vivo

Pharmacodynamics analysis reveals that E7090 inhibits phosphorylation of FGFRs in SNU-16 xenograft tumors in a dose-dependent manner. Overall, the in vitro and in vivo studies confirm that E7090 is a potent and selective FGFRs inhibitor, showing promising antitumor activities with wider therapeutic windows in preclinical cancer models harboring FGFRs gene abnormalities[1]. E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model[2.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mouse xenograft model of SNU-16 human gastric cancer[2].
Dosage: 6.25 to 50 mg/kg.
Administration: Orally, once daily for 14 days.
Result: Inhibited tumor growth in a dose-dependent manner.
Clinical Trial
Molecular Weight

764.82

Formula

C₃₂H₃₇N₅O₆.₃/₂C₄H₆O₄

CAS No.
SMILES

O=C(O)CCC(O)=O.O=C(N1C=CC2=C1C=C(OCCOC)C(OC3=CC(NC(C4=CC=C(C5CCN(CCO)CC5)C=C4)=O)=NC=C3)=C2)NC.[3/2]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

E7090E 7090E-7090FGFRFibroblast growth factor receptorSolidtumor4T1metastasisendometrialcancerMFE280AN3CAMFE296Inhibitorinhibitorinhibit

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Product Name:
E7090 succinate
Cat. No.:
HY-101466A
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