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

Famitinib malate  (Synonyms: SHR1020 malate)

Cat. No.: HY-108713A
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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.

Famitinib malate Chemical Structure

Famitinib malate Chemical Structure

CAS No. : 1256377-67-9

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Famitinib malate Related Antibodies

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Description

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[1][2].

IC50 & Target

VEGFR2

4.2 nM (IC50)

PDGFRβ

6.6 nM (IC50)

c-kit

2.3 nM (IC50)

In Vitro

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.

Famitinib malate 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 malate 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 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).
Clinical Trial
Molecular Weight

544.58

Formula

C27H33FN4O7
CAS No.
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.[(Z)]
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
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Famitinib malate Related Classifications

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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:

Famitinib1256377-67-9SHR1020SHR 1020SHR-1020VEGFRPDGFRApoptosisVascular endothelial growth factor receptorPlatelet-derived growth factor receptororalactivemulti-targetedkinaseantitumorgastricapoptosistyrosinecancerInhibitorinhibitorinhibit

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