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ASP5878

Catalog No. T5473 CAS 1453208-66-6

Synonyms: 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.

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ASP5878, CAS 1453208-66-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
2 mg	In stock	$ 138.00
5 mg	In stock	$ 213.00
10 mg	In stock	$ 347.00
25 mg	In stock	$ 589.00
50 mg	In stock	$ 842.00
100 mg	In stock	$ 1,160.00
1 mL * 10 mM (in DMSO)	In stock	$ 235.00

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Purity: 99.86%

Purity: 99.8%

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Storage & Solubility Information

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	FGFR4:3.5nM, FGFR3:0.74nM, FGFR1:0.47nM, FGFR2:0.6nM
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.

Synonyms	ASP-5878
Molecular Weight	407.37
Formula	C18H19F2N5O4
CAS No.	1453208-66-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (613.69 mM)

References and Literature

1. Futami T, et al. ASP5878, a Novel Inhibitor of FGFR1, 2, 3, and 4, Inhibits the Growth of FGF19-Expressing Hepatocellular Carcinoma. Mol Cancer Ther. 2017 Jan;16(1):68-75.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Orally Active Compound Library Bioactive Compound Library Angiogenesis related Compound Library

Related Products

Related compounds with same targets

FGFR1 inhibitor-10 KI8751 FGFR1/DDR2 inhibitor 1 FGFR4-IN-16 Dovitinib SKLB 610 PD173074 Roblitinib

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Keywords

ASP5878 1453208-66-6 Angiogenesis Tyrosine Kinase/Adaptors FGFR ASP-5878 Inhibitor ASP 5878 Fibroblast growth factor receptor inhibit inhibitor

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