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ASP5878
🥰Excellent
Catalog No. T5473Cas No. 1453208-66-6
Alias ASP-5878
ASP5878 potently inhibited the tyrosine kinase activities of recombinant FGFR1, 2, 3, and 4 with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L.
ASP5878
🥰Excellent
Purity: 99.86%
Catalog No. T5473Alias ASP-5878Cas No. 1453208-66-6
ASP5878 potently inhibited the tyrosine kinase activities of recombinant FGFR1, 2, 3, and 4 with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $60 | In Stock | |
| 5 mg | $163 | In Stock | |
| 10 mg | $247 | In Stock | |
| 25 mg | $446 | In Stock | |
| 50 mg | $625 | In Stock | |
| 100 mg | $876 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $179 | In Stock |
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Purity:99.86%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | ASP5878 potently inhibited the tyrosine kinase activities of recombinant FGFR1, 2, 3, and 4 with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L. |
| Targets&IC50 | FGFR1:0.47nM, FGFR2:0.6nM, FGFR3:0.74nM, FGFR4:3.5nM |
| In vivo | sorafenib administration for 14 days caused 40% tumor growth inhibition in the Hep3B2.1-7 xenograft model. Even after continuous sorafenib treatment, the Hep3B2.1-7 tumor gradually enlarged, and 47% tumor growth inhibition was observed by day 31. In contrast, the switch from sorafenib to ASP5878 on day 14 induced 83% tumor regression on day 52 relative to the tumor size observed on day 14. This indicates the therapeutic potential of ASP5878 for FGF19-overexpressing HCC patients who previously received sorafenib treatment. |
| Kinase Assay | Inhibitory activities of 128 serine/threonine kinases were measured using the Mobility Shift Assay Kit.?IC50 values were determined for kinases that were inhibited by more than 50% by 200 nmol/L of ASP5878. |
| Cell Research | The human HCC cell lines,?The experiments were conducted using low-passage cultures of these stocks.?The cells were seeded in 96-well plates and incubated overnight.?The cells were treated with ASP5878 for 5 days.?Cell viability was measured using CellTiter-Glo. |
| Animal Research | HuH-7-Luc cells were inoculated into hepatic parenchyma at 3×10^5 cells/0.01 mL (Matrigel 100%)/mouse.?One week after inoculation, the mice were divided into three groups (n = 5 per group) on day 0 on the basis of bioluminescent imaging.?Vehicle (Cremophor EL/ethanol or 0.5% MC), sorafenib (30 mg/kg), or ASP5878 (3 mg/kg) was administered as a once-daily oral dose for 91 days.?Tumor growth was monitored by in vivo bioluminescent imaging of the abdomen after intraperitoneally injecting luciferin using IVIS-Lumina2.?During the study period (181 days), the survival of mice bearing hepatic tumors was recorded.?The condition of the mice was monitored daily.?The mice were scored as dead if any of the following signs of suffering were observed: cachexia, weakening, and difficulty in moving or eating.?Mice that were scored as dead were euthanized. |
| Alias | ASP-5878 |
| Molecular Weight | 407.37 |
| Formula | C18H19F2N5O4 |
| Cas No. | 1453208-66-6 |
| Smiles | COc1cc(OC)c(F)c(COc2cnc(Nc3cnn(CCO)c3)nc2)c1F |
| Relative Density. | 1.41 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 250 mg/mL (613.69 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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