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

Famitinib (Synonyms: 法米替尼; SHR1020)

目录号: HY-108713
产品使用指南

Famitinib (SHR1020) 是一种有效的,具有口服活性的多靶点激酶抑制剂,抑制 c-kit, VEGFR-2PDGFRβ 的活性,IC50 值分别为 2.3 nM、4.7 nM 和 6.6 nM。Famitinib具有抗肿瘤活性。且诱导细胞凋亡 (apoptosis)。

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Famitinib Chemical Structure

Famitinib Chemical Structure

CAS No. : 1044040-56-3

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生物活性

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)

体外研究
(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.
体内研究
(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).
分子量

410.48

Formula

C23H27FN4O2

CAS 号
中文名称

法米替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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Famitinib
目录号:
HY-108713
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