1. Protein Tyrosine Kinase/RTK
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  3. ASP5878

ASP5878 

Cat. No.: HY-19983 Purity: 99.71%
Handling Instructions

ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity.

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

ASP5878 Chemical Structure

ASP5878 Chemical Structure

CAS No. : 1453208-66-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3300 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity[1].

IC50 & Target[1]

FGFR1

0.47 nM (IC50)

FGFR2

0.6 nM (IC50)

FGFR3

0.74 nM (IC50)

FGFR4

3.5 nM (IC50)

In Vitro

ASP5878 shows potent antiproliferative activity in most human HCC cell lines[1].
ASP5878 inhibits FGFR4 phosphorylation in a concentration-dependent manner. ASP5878 treatment results in the suppression of phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation[1].

Cell Viability Assay[1]

Cell Line: Human HCC cell lines.
Concentration: 0-1000 nM.
Incubation Time: 5 days.
Result: HuH-7, Hep3B2.1-7, and JHH-7 cell lines exhibited potent sensitivity to ASP5878, with IC50 values of 27, 8.5, and 21 nmol/L, respectively.
The growth inhibition rate of HLF was 64% and those of other ASP5878-sensitive cell lines were higher than 95% at 1000 nM.
In Vivo

ASP5878 (3 mg/kg, orally, once daily) shows antitumor activity in a Hep3B2.1-7 subcutaneous xenograft and HCC orthotopic xenograft mouse model[1].
ASP5878 induces shrinkage of FGF19-expressing HCC xenograft model[1].

Animal Model: Four-week-old male nude mice (CAnN.Cg-Foxn1nu/CrlCrlj [nu/nu]) (Hep3B2.1-7 cells inoculated subcutaneously)[1].
Dosage: 3 mg/kg.
Administration: Orally once daily from days 14 to 52.
Result: Induced tumor regression by 9% and 88% at 1 and 3 mg/kg, respectively, without affecting the body weight for 14 days.
Induced the suppression of FGFR4 phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation.
Animal Model: HCC orthotopic xenograft model (mouse)[1].
Dosage: 3 mg/kg.
Administration: Orally once daily for 24 days.
Result: Exhibited a lower tumor burden than vehicle- and sorafenibtreated mice.
Induced sustained tumor regression without tumor regrowth.
Clinical Trial
Molecular Weight

407.37

Formula

C₁₈H₁₉F₂N₅O₄

CAS No.

1453208-66-6

SMILES

OCCN1N=CC(NC2=NC=C(OCC3=C(F)C(OC)=CC(OC)=C3F)C=N2)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (613.69 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4548 mL 12.2739 mL 24.5477 mL
5 mM 0.4910 mL 2.4548 mL 4.9095 mL
10 mM 0.2455 mL 1.2274 mL 2.4548 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
ASP5878
Cat. No.:
HY-19983
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