Esuberaprost Sodium

Product Name: Esuberaprost Sodium
CAS No.: 1044040-56-3
Chemical Name: Esuberaprost Sodium
Synonyms: (Z)-Famitinib;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-
CBNumber: CB93159898
Molecular Formula: C23H27FN4O2
Formula Weight: 410.4844832
MOL File: 1044040-56-3.mol

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Esuberaprost Sodium Property

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

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Hazard and Precautionary Statements (GHS)

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Esuberaprost Sodium Chemical Properties,Usage,Production

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

Esuberaprost Sodium Preparation Products And Raw materials

Raw materials

Preparation Products

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Esuberaprost Sodium Suppliers

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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

1044040-56-3