1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. FR 111142

FR 111142 is an angiogenesis inhibitor (IC50 = 18.4 μM) and has anti-inflammatory activity (IC50 = 20.6 μM). FR 111142 inhibits capillary-like tube formation as well as nitric oxide production in LPS (HY-D1056)-activated murine macrophages. FR 111142 enhances catabolism of low-density lipoprotein (LDL). FR 111142 does not induce significant cytotoxicity in human endothelial progenitor cells, nor affect cell viability of murine macrophages. FR 111142 can be used for the research of cancer, inflammatory diseases.

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FR 111142

FR 111142 Chemical Structure

CAS No. : 132340-44-4

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Description

FR 111142 is an angiogenesis inhibitor (IC50 = 18.4 μM) and has anti-inflammatory activity (IC50 = 20.6 μM). FR 111142 inhibits capillary-like tube formation as well as nitric oxide production in LPS (HY-D1056)-activated murine macrophages. FR 111142 enhances catabolism of low-density lipoprotein (LDL). FR 111142 does not induce significant cytotoxicity in human endothelial progenitor cells, nor affect cell viability of murine macrophages. FR 111142 can be used for the research of cancer, inflammatory diseases[1][2][3].

Cellular Effect
Cell Line Type Value Description References
RAW264.7 IC50
20.6 μM
Compound: FR-111142
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production compound treated prior to LPS challenge by Griess assay
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production compound treated prior to LPS challenge by Griess assay
[PMID: 27976895]
In Vitro

FR 111142 (10-20 μM; 24 h) inhibits capillary tube formation in human endothelial progenitor cells with an IC50 of 18.4 μM without causing cytotoxicity at 20 μM[1].
FR 111142 (up to 100 μM) completely inhibits LPS-induced NO production in RAW264.7 cells with an IC50 of 20.6 μM without reducing cell viability at concentrations up to 100 μM[1].
FR 111142 is effective against HUVEC cell and EL-4 cell with IC50s of 5.0 × 10-4 μg/mL and 3.8 × 10-4 μg/mL, respectively[2].
FR 111142 (10-40 μM; 5-25 h) enhances the catabolism of LDL in HepG2 cells[3].

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

Cell Cytotoxicity Assay[1]

Cell Line: human endothelial progenitor cells
Concentration: 10 μM; 20 μM
Incubation Time: 24 h
Result: Inhibited capillary tube formation with an IC50 of 18.4 μM without causing cytotoxicity at 20 μM.
In Vivo

FR-111142 (0.3-30 mg/kg/d; i.v.; qd 1-4 and 7-10 d) is quite active against tumor in female Balb/c mice implanted intradermally at an inoculum size of 1 x 105 Meth A cells[2].

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

Animal Model: Balb/c mice (female;
8 weeks old; implanted intradermally at an inoculum size of 1 x 105 Meth A cells per mouse for fibrosarcoma model)
[2]
Dosage: 30 mg/kg/day; 10 mg/kg/day; 3.3 mg/kg/day; 1.0 mg/kg/day; 0.3 mg/kg/day
Administration: i.v.; qd 1-4 and 7-10 d
Result: Significant suppressed tumor growth at 3.3~30mg/kg.
Molecular Weight

410.50

Formula

C22H34O7

CAS No.
SMILES

O=C(/C=C/[C@H]([C@H](C)O)O)O[C@H]1CC[C@@]2([C@@]([C@@]3(C)O[C@H]3C/C=C(C)\C)([H])[C@H]1OC)OC2

Structure Classification
Initial Source

Phoma sp. NTOU4195

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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References
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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.

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Product Name:
FR 111142
Cat. No.:
HY-182569
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