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.
For research use only. We do not sell to patients.
- CAS No.: 132340-44-4
- Formula: C22H34O7
- Molecular Weight:410.50
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All VEGFR Isoforms
More
Biological Activity
|
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] |
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 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.
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.
Chemical Information
-
CAS No. 132340-44-4
-
Molecular Weight 410.50
-
Formula C22H34O7
-
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.
Purity & Documentation
References
[1]. Lee MS, et al. Angiogenesis Inhibitors and Anti-Inflammatory Agents from Phoma sp. NTOU4195. J Nat Prod. 2016;79(12):2983-2990. [Content Brief]
[2]. Otsuka T, et al. A new angiogenesis inhibitor, FR-111142. J Antibiot (Tokyo). 1992 Mar;45(3):348-54. [Content Brief]
[3]. Harada T, et al. Induction of low-density lipoprotein catabolism in Hep G2 cells by a fungal sesquiterpene ester, FR111142. Biochem Biophys Res Commun. 1998 Oct 29;251(3):830-4 [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz