| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
IC50: 0.4 μM (Heparanase)[1]
OGT2115 targets heparanase, an endoglycosidase that cleaves heparan sulfate side chains of heparan sulfate proteoglycans in the extracellular matrix. Heparanase activity is involved in extracellular matrix remodeling, angiogenesis, and tumor metastasis. By inhibiting heparanase, OGT2115 disrupts these processes. The compound displays no major inhibition of human cytochrome P450 isoenzymes. |
|---|---|
| ln Vitro |
OGT 2115 has a negligible but noticeable effect on the spread of breast cancer cells caused by endoplasmic reticulum (ER) stress. When cells were treated to Tunicamycin + OGT 2115, however, the quantity and rate of migrating cells were considerably lower than in the control group. The invasion and migration caused by doxorubicin were dramatically suppressed by OGT 2115. Additionally, OGT 2115 did not lessen the antiproliferative impact of doxorubicin, according to the results of the MTT experiment [2].
In vitro, OGT2115 acts as a potent heparanase inhibitor with an IC₅₀ of 0.4 µM. It also inhibits angiogenesis with an IC₅₀ of 7.5 µM. Its in vitro activity is assessed using biochemical assays that measure heparanase activity and cell-based assays that assess angiogenesis. |
| ln Vivo |
Following oral administration of 20 mg/kg, OGT 2115 (Compound 12d) demonstrated plasma concentrations in mice that were almost ten times higher than those of heparanase [1].
In vivo activity of OGT2115 has been demonstrated in preclinical models of angiogenesis and tumor growth. As an orally active compound, it is suitable for oral administration. Its anti-angiogenic properties support its use in cancer research. In vivo efficacy is assessed by measuring inhibition of angiogenesis and tumor growth. |
| Enzyme Assay |
The in vitro enzyme assay for OGT2115 involves measuring its inhibitory activity against heparanase in cell-free systems. These assays use purified heparanase enzyme and measure the cleavage of heparan sulfate substrates in the presence of the compound. Inhibitory potency is determined by assessing the IC₅₀ (0.4 µM). Cytochrome P450 inhibition is also assessed.
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| Cell Assay |
In vitro cellular assays for OGT2115 are performed using various cell types, including endothelial cells and cancer cells. These assays measure the compound's ability to inhibit heparanase activity, reduce extracellular matrix remodeling, and inhibit angiogenesis. The compound's cell permeability enables its use in these assays.
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| Animal Protocol |
In vivo animal studies for OGT2115 are conducted in models of angiogenesis and tumor growth. These studies typically involve oral administration of the compound, followed by assessment of angiogenesis, tumor growth, and metastasis. The compound's oral bioavailability supports its use in these models.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of OGT2115 are characterized by oral bioavailability and cell permeability. The compound has a molecular formula of C₂₄H₁₆BrFN₂O₄ and a molecular weight of 495.30 g/mol. Its pharmacokinetic profile supports oral dosing for research applications.
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| Toxicity/Toxicokinetics |
Toxicology studies of OGT2115 have been conducted to support its use in preclinical research. As a heparanase inhibitor, its toxicology profile includes effects on extracellular matrix remodeling and angiogenesis in normal tissues. The compound displays no major inhibition of human cytochrome P450 isoenzymes, suggesting a favorable drug-drug interaction profile.
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| References |
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| Additional Infomation |
OGT2115 (CAS: 853929-59-6) is a potent, cell-permeable, and orally active heparanase inhibitor with an IC₅₀ of 0.4 µM. It also inhibits angiogenesis with an IC₅₀ of 7.5 µM. The compound has a molecular formula of C₂₄H₁₆BrFN₂O₄ and a molecular weight of 495.30 g/mol. It is for research use only.
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| Molecular Formula |
C24H16BRFN2O4MOLECULARWEIGHT
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|---|---|
| Molecular Weight |
495.3044
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| Exact Mass |
494.027
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| CAS # |
853929-59-6
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| PubChem CID |
44402523
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| Appearance |
White to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
685.9±55.0 °C at 760 mmHg
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| Flash Point |
368.6±31.5 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.710
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| LogP |
6.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
700
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1/C=C/C(=O)NC2=C(C=C(C=C2)C3=NC4=C(O3)C=CC(=C4)CC(=O)O)F)Br
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| InChi Key |
LKBXWNYXDMSFQU-ONNFQVAWSA-N
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| InChi Code |
InChI=1S/C24H16BrFN2O4/c25-17-6-1-14(2-7-17)4-10-22(29)27-19-8-5-16(13-18(19)26)24-28-20-11-15(12-23(30)31)3-9-21(20)32-24/h1-11,13H,12H2,(H,27,29)(H,30,31)/b10-4+
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| Chemical Name |
2-[2-[4-[[(E)-3-(4-bromophenyl)prop-2-enoyl]amino]-3-fluorophenyl]-1,3-benzoxazol-5-yl]acetic acid
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| Synonyms |
OGT2115; OGT2115; OGT -115
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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 : ~11.36 mg/mL (~22.94 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.14 mg/mL (2.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.4 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 10 mg/mL (20.19 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O 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 | 2.0190 mL | 10.0949 mL | 20.1898 mL | |
| 5 mM | 0.4038 mL | 2.0190 mL | 4.0380 mL | |
| 10 mM | 0.2019 mL | 1.0095 mL | 2.0190 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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