Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
EG-00229 TFA, the trifluoroacetic acid form of EG00229, is a novel and potent Neuropilin 1 (NRP1) receptor antagonist with antitumor effects. It selectively inhibits 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 |
After 48 hours of incubation, treatment with EG00229 (Compound 2; 0-100 μM; 48 hours; A549 cells) significantly reduced the viability of the cells [1]. Compound 2 (EG00229) reduces endothelial cell VEGFR2 phosphorylation and prevents VEGF-A from attaching to NRP1. HUVEC have also shown evidence of inhibition of endothelial cell migration [1]. At an IC50 of 8 μM, EG00229 (compound 2) specifically prevents radiolabeled 125I-VEGF-A from binding to porcine aortic endothelium (PAE)/NRP1, but not to VEGFR2-expressing cells. EG00229 similarly decreased VEGF-A binding to prostate cancer DU145 and lung cancer A549 cells, which express NRP1 but not VEGFR1 or VEGFR2. EG00229, with an IC50 of 23 μM, also inhibits the binding of VEGF-A to human umbilical vein endothelial cells (HUVEC) expressing VEGFR2, VEGFR1, and NRP1 [1].
|
---|---|
ln Vivo |
For four weeks, NSG mice treated with EG00229 (0–10 mg/kg; i.p.; three times per week) showed a significant decrease in tumor growth and evident vascularization [2].
|
Cell Assay |
Cell Viability Assay[1]
Cell Types: A549 Cell Tested Concentrations: 0 µM, 10 µM, 30 µM, 100 µM Incubation Duration: 48 hrs (hours) Experimental Results: Caused significant reduction in cell viability. |
Animal Protocol |
Animal/Disease Models: 6weeks 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; every Wednesday times; lasts 4 weeks Experimental Results: diminished tumor growth and visible blood vessel formation. |
References |
[1]. Jarvis A, et al. Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction. J Med Chem. 2010 Mar 11;53(5):2215-26.
[2]. Grun D, et al. VEGF-A acts via neuropilin-1 to enhance epidermal cancer stem cell survival and formation of aggressive and highly vascularized tumors. Oncogene. 2016 Aug 18;35(33):4379-87. |
Molecular Formula |
C₁₉H₂₀F₃N₇O₇S₃
|
---|---|
Molecular Weight |
611.595
|
CAS # |
1210945-69-9
|
Related CAS # |
1018927-63-3;1210945-69-9 (TFA);
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
O=S(C1=CC=CC2=NSN=C12)(NC3=C(C(N[C@H](C(O)=O)CCCNC(N)=N)=O)SC=C3)=O.FC(F)(F)C(O)=O
|
InChi Key |
ZYQBITUOSRZDTG-MERQFXBCSA-N
|
InChi Code |
InChI=1S/C17H19N7O5S3.C2HF3O2/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)23-31-22-93-2(4,5)1(6)7/h1,3,5-6,8,11,24H,2,4,7H2,(H,21,25)(H,26,27)(H4,18,19,20)(H,6,7)/t11-/m0./s1
|
Chemical Name |
N2-[[3-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-2-thienyl]carbonyl]-L-arginine trifluoroacetate
|
Synonyms |
EG 00229 trifluoroacetate, EG-00229 TFA, EG-00229 trifluoroacetate, EG00229 TFA,
EG00229 trifluoroacetate, EG 00229 TFA
|
HS Tariff Code |
2934.99.9001
|
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)
|
Solubility (In Vitro) |
DMSO : ≥ 41.4 mg/mL (~67.69 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.09 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6351 mL | 8.1753 mL | 16.3506 mL | |
5 mM | 0.3270 mL | 1.6351 mL | 3.2701 mL | |
10 mM | 0.1635 mL | 0.8175 mL | 1.6351 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.