Esuberaprost Sodium
Esuberaprost Sodium Basic information
- Product Name:
- Esuberaprost Sodium
- Synonyms:
-
- Esuberaprost Sodium
- 4H-Pyrrolo[3,2-c]pyridin-4-one, 5-[2-(diethylamino)ethyl]-2-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-1,5,6,7-tetrahydro-3-methyl-
- (Z)-Famitinib
- CAS:
- 1044040-56-3
- MF:
- C23H27FN4O2
- MW:
- 410.4844832
- Mol File:
- 1044040-56-3.mol
Esuberaprost Sodium Chemical Properties
- Boiling point:
- 677.1±55.0 °C(Predicted)
- Density
- 1.271±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- pka
- 11.73±0.20(Predicted)
- form
- Solid
- color
- Yellow to orange
Esuberaprost Sodium Usage And Synthesis
Uses
Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively[1]. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis[2].
in vivo
Famitinib exhibits broad and potent anti-tumor activity, leading to regression or growth arrest of various established xenografts derived from human tumor cell lines [1].
Famitinib (50 and 100 mg/kg; p.o. once daily for 3 weeks) reduces tumor growth in vivo via inhibition of angiogenesis[2].
| Animal Model: | 18-20 g female BALB/c athymic?nu/nu?mice (age, 6–8 weeks) bearing BGC-823 xenografts[2] |
| Dosage: | 50 and 100 mg/kg |
| Administration: | Oral gavage; 50 and 100 mg/kg; once daily for 3 weeks |
| Result: | Inhibited BGC-823 xenograft growth (tumor volume, 395.2 vs. 2,690.5 mm3), and animal weights were similar between groups (21.6 vs. 18.7 g). |
IC 50
VEGFR-2: 4.2 nM (IC50); PDGFRβ: 6.6 nM (IC50); c-kit: 2.3 nM (IC50)
References
[1] Liguang?Lou,?et al. Abstract 3604: Preclinical antitumor study of famitinib, an orally available multi-targeted kinase inhibitor of VEGFR/PDGFR/c-Kit in phase I clinical trials.
[2] Sai Ge, et al. Famitinib exerted powerful antitumor activity in human gastric cancer cells and xenografts. Oncol Lett.?2016 Sep;12(3):1763-1768. DOI:10.3892/ol.2016.4909
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