1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. VEGFR
    PDGFR
    Apoptosis
  3. Famitinib

Famitinib (Synonyms: SHR1020)

Cat. No.: HY-108713
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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. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis.

For research use only. We do not sell to patients.

Famitinib Chemical Structure

Famitinib Chemical Structure

CAS No. : 1044040-56-3

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Description

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].

IC50 & Target[2]

VEGFR-2

4.2 nM (IC50)

PDGFRβ

6.6 nM (IC50)

c-kit

2.3 nM (IC50)

In Vitro

Famitinib inhibits the VEGF-induced proliferation, migration and tubule formation of human umbilical vein endothelial cells, and micro-vessel spouting from matrigel-embedded rat aortic rings[1].
Famitinib inhibits cell proliferation by inducing cell cycle arrest at the G2/M phase and causes cell apoptosis in a dose-dependent manner in gastric cancer cell lines. Famitinib (0.6-20.0 µM) inhibits gastric cancer cell growth in a dose-dependent manner[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[3]

Cell Line: Human gastric cancer cells BGC-823 and MGC-803
Concentration: 0, 0.6, 1.25, 2.5, 5.0, 10.0 and 20.0 µM
Incubation Time: 24, 48 and 72 hours
Result: Inhibited cell growth in a dose-dependent manner. The IC50 values in BGC-823 and MGC-803 cells were 3.6 and 3.1 µM, respectively.
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 significantly slows tumor growth in vivo via inhibition of angiogenesis in BGC-823 xenograft models. Famitinib (50 and 100 mg/kg;gavage) reduces xenograft growth in vivo via inhibition of angiogenesis[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 18-20 g female BALB/c athymic nu/nu mice (age, 6–8 weeks) bearing BGC-823 xenografts[4]
Dosage: 50 and 100 mg/kg
Administration: Gavage, once daily for 3 weeks
Result: Both doses exerted a similar inhibitory power, but greater toxicity was observed.
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).
Molecular Weight

410.48

Formula

C₂₃H₂₇FN₄O₂

CAS No.
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Famitinib
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