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

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.

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Famitinib Chemical Structure

Famitinib Chemical Structure

CAS No. : 1044040-56-3

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Based on 1 publication(s) in Google Scholar

Other Forms of Famitinib:

Famitinib Related Antibodies

Top Publications Citing Use of Products

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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PDGFR PDGFRβ PDGFRα

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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 (1.8 and 3.6 μM; 48 h) 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[2].
Famitinib (0.6-20.0 µM; 24-72 h) inhibits gastric cancer cell growth in a dose-dependent manner[2].

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

Famitinib Related Antibodies

Cell Proliferation Assay[2]

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 with IC50 values of 3.6 and 3.1 µM for BGC-823 and MGC-803 cells, 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 (50 and 100 mg/kg; p.o. once daily for 3 weeks) reduces tumor growth in vivo via inhibition of angiogenesis[2].

MedChemExpress (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[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).
Clinical Trial
Molecular Weight

410.48

Formula

C23H27FN4O2
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C1C2=C(NC(/C=C3C(NC4=C\3C=C(F)C=C4)=O)=C2C)CCN1CCN(CC)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 4.17 mg/mL (10.16 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4362 mL 12.1809 mL 24.3617 mL
5 mM 0.4872 mL 2.4362 mL 4.8723 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4362 mL 12.1809 mL 24.3617 mL 60.9043 mL
5 mM 0.4872 mL 2.4362 mL 4.8723 mL 12.1809 mL
10 mM 0.2436 mL 1.2181 mL 2.4362 mL 6.0904 mL
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Famitinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Famitinib1044040-56-3SHR1020SHR 1020SHR-1020VEGFRPDGFRApoptosisVascular endothelial growth factor receptorPlatelet-derived growth factor receptorOrallyactivemulti-targetedkinaseantitumorgastricapoptosistyrosinecancerInhibitorinhibitorinhibit

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