| Size | Price | Stock | Qty |
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| Targets |
IMS2186 targets angiogenesis and cell cycle progression. It inhibits angiogenesis upstream of VEGF, blocking the formation of new blood vessels. It arrests cancer cell cycle in G2/M phase, thereby exerting anti-proliferation effects. It also inhibits the production of PGE2/TNF-α. Its multi-target mechanism contributes to its anti-proliferative and anti-angiogenic effects.
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| ln Vitro |
Human fibroblasts and human cancer cells proliferate at IMS2186 (0.3-10 μM; 22 h); their corresponding IC50 values are 1.0-3.0 μM and 0.3-3.0 μM[1]. With an IC50 of 0.1-0.3 μM, IMS2186 (0-10 μM; 22 h) suppresses the production of the pro-inflammatory cytokine PGE2/TNF-a in macrophages [1]. With an IC50 of 1 μM, IMS2186 (0.1-10 μM; 1.5 h) similarly prevents macrophage migration [1].
IMS2186 is an anti-proliferative and anti-angiogenic compound. It inhibits angiogenesis upstream of VEGF and can arrest cancer cell cycle in G2/M phase. It inhibits cell growth in vitro in tumor cells, non-transformed fibroblasts, and retinal pigment epithelial cells. Its activity has been confirmed in various in vitro and in vivo studies. |
| ln Vivo |
No ocular toxicity was seen following delivery of IMS2186 (2.5 mg in 0.5 mL; intravitreal injection; single dose) to the eye [1]. IMS2186 (100 μg/eye, i.e. 2.0 μL of 50 μg/μL solution; single dosage) displays anti-aging effects in a vascular model of laser-induced choroidal neovascularization (CNV) [1].
IMS2186 is an anti-choroidal neovascularization (CNV) agent that inhibits angiogenesis upstream of VEGF. It can arrest cancer cell cycle in G2/M phase, thus exerting anti-proliferation and anti-angiogenesis effects. It reduces eye leakage and the number of lesion cells without intraocular toxicity. It has potential applications in the treatment of CNV and cancer. |
| Enzyme Assay |
The primary in vitro assays for IMS2186 include cell proliferation assays using various cell lines, such as tumor cells, fibroblasts, and retinal pigment epithelial cells. Cell viability is measured using MTT or similar assays. The compound's effects on cell cycle distribution are assessed by flow cytometry. Its anti-angiogenic activity is assessed using endothelial cell tube formation assays or aortic ring assays.
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| Cell Assay |
Cell cycle analysis[1]
Cell Types: Cancer H460 cells Tested Concentrations: 3 μM 0.3-1 μM[1]. , 10 μM Incubation Duration: Experimental Results: Demonstrates anti-proliferative activity mediated by arresting the cell cycle at G2/M. In vitro cellular experiments for IMS2186 involve treating cells with the compound and measuring its effects on cell proliferation, cell cycle progression, and angiogenesis. The inhibition of VEGF-induced angiogenesis is assessed in endothelial cell cultures. The compound's effects on PGE2 and TNF-α production are measured by ELISA. |
| Animal Protocol |
Animal/Disease Models: Laser-induced CNV rat model [1]
Doses: 100 μg/eye, 50 μg/eye solution 2.0 μL μL Route of Administration: intravitreal injection; single dose Experimental Results: in lesion area measurement, compared with PBS The area has been diminished by 30%. In vivo animal experiments for IMS2186 have been conducted in models of choroidal neovascularization (CNV) to assess its anti-angiogenic effects. It could also be evaluated in tumor xenograft models to assess its anti-proliferative effects. Its effects on angiogenesis and tumor growth would be assessed. |
| ADME/Pharmacokinetics |
IMS2186 has a molecular weight of 296.32 and a molecular formula of C18H16O4. It is an anti-choroidal neovascularization (CNV) agent. The compound has a CAS number of 1031206-36-6. It inhibits angiogenesis upstream of VEGF and arrests cancer cell cycle in G2/M phase.
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| Toxicity/Toxicokinetics |
IMS2186 is a research compound that is not intended for human use. Its toxicological profile is not extensively characterized in the available literature. It is reported to reduce eye leakage and the number of lesion cells without intraocular toxicity. As with all research chemicals, standard safety precautions should be followed when handling.
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| References |
[1]. Falkenstein IA, et al. Toxicity and intraocular properties of a novel long-acting anti-proliferative and anti-angiogenic compound IMS2186. Curr Eye Res. 2008 Jul;33(7):599-609.
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| Additional Infomation |
IMS2186 is an anti-proliferative and anti-angiogenic compound that inhibits angiogenesis upstream of VEGF. It is an anti-choroidal neovascularization (CNV) agent that can arrest cancer cell cycle in G2/M phase. It inhibits cell growth in vitro in tumor cells, fibroblasts, and retinal pigment epithelial cells.
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| Molecular Formula |
C18H16O4
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| Molecular Weight |
296.317245483398
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| Exact Mass |
296.105
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| CAS # |
1031206-36-6
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| PubChem CID |
24987039
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.367
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
444
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC2=C(C=C1)OCC(=CC3=CC(=C(C=C3)OC)O)C2=O
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| InChi Key |
BZCADTHMZLYKAR-MDWZMJQESA-N
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| InChi Code |
InChI=1S/C18H16O4/c1-11-3-5-16-14(7-11)18(20)13(10-22-16)8-12-4-6-17(21-2)15(19)9-12/h3-9,19H,10H2,1-2H3/b13-8+
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| Chemical Name |
(3E)-3-[(3-hydroxy-4-methoxyphenyl)methylidene]-6-methylchromen-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~66.67 mg/mL (~224.99 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (4.22 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3747 mL | 16.8737 mL | 33.7473 mL | |
| 5 mM | 0.6749 mL | 3.3747 mL | 6.7495 mL | |
| 10 mM | 0.3375 mL | 1.6874 mL | 3.3747 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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