Famitinib malate
Famitinib (SHR1020) malate, 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 malate induces cell apoptosis. Famitinib malate exerts powerful antitumor activity in human gastric cancer cells and xenografts, it can be used for the research of cancer.
For research use only. We do not sell to patients.
- CAS No.: 1256377-67-9
- Formula: C27H33FN4O7
- Molecular Weight:544.58
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All VEGFR Isoforms
More
Biological Activity
|
VEGFR2 4.2 nM (IC50) |
PDGFRβ 6.6 nM (IC50) |
c-kit 2.3 nM (IC50) |
Famitinib malate 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 malate (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 malate (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.
-
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.
Famitinib malate (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).
Chemical Information
-
CAS No. 1256377-67-9
-
Molecular Weight 544.58
-
Formula C27H33FN4O7
-
SMILES
O=C1C2=C(NC(/C=C3C(NC4=C\3C=C(F)C=C4)=O)=C2C)CCN1CCN(CC)CC.O[C@H](C(O)=O)CC(O)=O
-
Synonyms
SHR1020 malate
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Famitinib malate Related Classifications
HY-108713A Related Classifications
Powered by Bioz