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50mg | ||
100mg | ||
250mg | ||
500mg |
Purity: ≥98%
EG00229 (EG-00229) is a novel and potent Neuropilin 1 (NRP1) receptor antagonist with anticancer activity. It acts by selectively inhibiting VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2. EG00229 inhibits VEGFA binding to NRP1.
ln Vitro |
Over the course of a 48-hour incubation, treatment with EG00229 (Compound 2; 0-100 μM; A549 cells) significantly reduces cell viability[1]. In endothelial cells, EG00229 (Compound 2) exhibits a reduction in VEGFR2 phosphorylation and a suppression of VEGF-A binding to NRP1. HUVECs have also been shown to inhibit endothelial cell migration[1]. Compound 2, EG00229, exhibits a selectivity of 8 μM in inhibiting radiolabeled 125I-VEGF-A binding to porcine aortic endothelial (PAE)/NRP1 cells, but not effecting VEGFR2-expressing cells. Moreover, EG00229 similarly and potently blocks VEGF-A binding to NRP1-expressing lung carcinoma A549 and prostate cancer DU145 cells, but not to VEGFR1 or VEGFR2. EG00229, with an IC50 of 23 μM, also inhibits the binding of VEGF-A to human umbilical vein endothelial cells (HUVECs), which express VEGFR2, VEGFR1, and NRP1[1].
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ln Vivo |
The intraperitoneal injection of EG00229 (0-10 mg/kg) administered three times a week for four weeks to NSG mice significantly inhibits tumor growth and evident vascularization[2].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: A549 cells Tested Concentrations: 0 µM, 10 μM, 30 μM, 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: Caused a significant reduction in cell viability. |
Animal Protocol |
Animal/Disease Models: 6-week old female NOD scid IL2 receptor gamma chain knockout mice (NSG mice) with ECS cells[2]
Doses: 0 mg/kg, 10 mg/kg Route of Administration: intraperitoneal (ip)injection; three times per week; for 4 weeks Experimental Results: Reduces tumor growth and visible vascularization. |
References |
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Molecular Formula |
C17H19N7O5S3
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Molecular Weight |
497.571658372879
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CAS # |
1018927-63-3
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Related CAS # |
1018927-63-3;1210945-69-9 (TFA);
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SMILES |
N=C(N)NCCC[C@@H](C(O)=O)NC(C1=C(NS(=O)(C2=CC=CC3=NSN=C32)=O)C=CS1)=O
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InChi Key |
ZWWMEDURALZMEV-NSHDSACASA-N
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InChi Code |
InChI=1S/C17H19N7O5S3/c18-17(19)20-7-2-4-11(16(26)27)21-15(25)14-10(6-8-30-14)24-32(28,29)12-5-1-3-9-13(12)23-31-22-9/h1,3,5-6,8,11,24H,2,4,7H2,(H,21,25)(H,26,27)(H4,18,19,20)/t11-/m0/s1
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Chemical Name |
(3-(benzo[c][1,2,5]thiadiazole-4-sulfonamido)thiophene-2-carbonyl)-L-arginine
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Synonyms |
EG00229 EG-00229 EG 00229
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0098 mL | 10.0488 mL | 20.0977 mL | |
5 mM | 0.4020 mL | 2.0098 mL | 4.0195 mL | |
10 mM | 0.2010 mL | 1.0049 mL | 2.0098 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.