[CAS NO. 1453208-66-6] ASP5878
PRODUCTS SPECIFICATIONS [1453208-66-6]
DESCRIPTION [1453208-66-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 407.37 |
| Molecular Formula | C18H19F2N5O4 |
| SMILES | OCCN1N=CC(NC2=NC=C(OCC3=C(F)C(OC)=CC(OC)=C3F)C=N2)=C1 |
Summary
IC50 & Target
|
FGFR1 0.47 nM (IC 50 ) |
FGFR2 0.6 nM (IC 50 ) |
FGFR3 0.74 nM (IC 50 ) |
FGFR4 3.5 nM (IC 50 ) |
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 IC
50
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02038673 | Astellas Pharma Inc|Astellas Pharma Global Development, Inc. |
Solid Tumors
|
November 5, 2013 | Phase 1 |
Appearance
Solid
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
DMSO : ≥ 250 mg/mL ( 613.69 mM )
* "≥" means soluble, but saturation unknown.
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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution