1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. CPL304110

CPL304110 

Cat. No.: HY-131908
Handling Instructions

CPL304110 is a potent, orally active and selective inhibitor of fibroblast growth factor receptors FGFR (1-3), with IC50 values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively.

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

CPL304110 Chemical Structure

CPL304110 Chemical Structure

CAS No. : 1627826-19-0

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Description

CPL304110 is a potent, orally active and selective inhibitor of fibroblast growth factor receptors FGFR (1-3), with IC50 values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively[1].

IC50 & Target[1]

FGFR1

0.75 nM (IC50)

FGFR2

0.5 nM (IC50)

FGFR3

3.05 nM (IC50)

In Vitro

CPL304110 (0-0.6 μM) dose-dependently inhibits FGFR2 phosphorylation and downstream signaling (p-ERK)[1].
CPL304110 (compound 56q) exhibits in SNU-16 proliferation assay with an IC50 of 85.64 nM[1].
CPL304110 (compound 56q) demonstrats a more than 45-fold, 345-fold, 395-fold and 680-fold selectivity over KDR (VEGFR2), Flt3, Aura A and PDGFRb, respectively relative to FGFR2, and no significant inhibitory effects were observed with other tyrosine kinases[1].

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

Western Blot Analysis[1]

Cell Line: SNU-16 cell lines.
Concentration: 0-0.6 μM.
Incubation Time: 1 h.
Result: Suppressed FGFR2 phosphorylation and downstream signaling (p-ERK)
In Vivo

CPL304110 (p.o., 40 mg/kg) exhibits a t1/2 of 2 h and Cmax of 3369 ng/mL in mice[1].
CPL304110 (compound 56q, 2 X 20 mg/kg) significantly inhibits tumor growth in mice without significant body loss or any toxicity. On day 21 (D21, day of termination) the tumor growth inhibition (TGI) is 64% for dosing 20 mg/kg twice a day[1].

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

Animal Model: Severe combined immunodeficient (SCID) mice implanted subcutaneously with SNU-16 (human)[1].
Dosage: 20 mg/kg (X2).
Administration: Orally, twice daily for 21 days.
Result: After 6 hours of last dosing, concentration of 56q decreased in the plasma (9%) but increased stepwise in the tumor cells (121%).
Clinical Trial
Molecular Weight

446.54

Formula

C₂₅H₃₀N₆O₂

CAS No.

1627826-19-0

SMILES

CN(CC1)CCN1C2=CC3=C(N=C(C4=NNC(CCC5=CC(OC)=CC(OC)=C5)=C4)N3)C=C2

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:

CPL304110CPL 304110CPL-304110FGFRFibroblast growth factor receptorLowtoxicityanti-tumorSNU-16Inhibitorinhibitorinhibit

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CPL304110
Cat. No.:
HY-131908
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