| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| ln Vitro |
EG01377 (3-30 μM; 30 minutes) suppresses the tyrosine phosphorylation of VEGF-R2/KDR induced by vascular endothelial growth factor A (VEGF-A) [1]. The migration of HUVEC cells in response to VEGFA can be considerably inhibited by EG01377 (30 μM) [1]. VEGF-induced wound closure is delayed by EG01377 (30 μM; 5 days) [1]. The network area, length, and branch points are all reduced by EG01377 (30 μM) [1]. VEGF-induced angiogenesis is decreased by EG01377 (30 μM; 7 days) [1]. A375P (malignant melanoma) spheroid growth is inhibited by EG01377 (30 μM; 7 days) in combination with VEGFA [1]. When tumor cell-derived factors are present, the synthesis of transforming growth factor beta (TGFβ) by Nrp1+ regulatory T cells SMAD3/AKT (Treg) is inhibited by EG01377 (500 nM; 2 hours) [1].
|
|---|---|
| ln Vivo |
The half-life of EG01377 (2 mg/kg; i.v.) is encouraging at 4.29 hours, which is sufficient to sustain once-daily dosing in mice [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: Human umbilical vein endothelial cells (HUVEC) Tested Concentrations: 3, 10, 30 μM Incubation Duration: 30 minutes Experimental Results: Inhibition of VEGF-A-stimulated VEGF-R2/KDR tyrosine phosphorylation, IC50 is 30 microns. |
| Animal Protocol |
Animal/Disease Models: 6-8 weeks old BABL/c female mice [1]
Doses: 2 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: intravenous (iv) (iv)injection Experimental Results: half-life (T1/2) is 4.29 h. |
| References |
| Molecular Formula |
C26H30N6O6S2
|
|---|---|
| Exact Mass |
586.166
|
| CAS # |
2227996-00-9
|
| Related CAS # |
EG01377 dihydrochloride;2749438-61-5
|
| PubChem CID |
133081972
|
| Appearance |
White to off-white solid
|
| LogP |
-0.7
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
40
|
| Complexity |
1010
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C1COC2=C1C=C(C=C2S(=O)(=O)NC3=C(SC=C3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C4=CC=C(C=C4)CN
|
| InChi Key |
SEXUXSMBJLNXIR-FQEVSTJZSA-N
|
| InChi Code |
InChI=1S/C26H30N6O6S2/c27-14-15-3-5-16(6-4-15)18-12-17-7-10-38-22(17)21(13-18)40(36,37)32-19-8-11-39-23(19)24(33)31-20(25(34)35)2-1-9-30-26(28)29/h3-6,8,11-13,20,32H,1-2,7,9-10,14,27H2,(H,31,33)(H,34,35)(H4,28,29,30)/t20-/m0/s1
|
| Chemical Name |
(2S)-2-[[3-[[5-[4-(aminomethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid
|
| 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 |
| 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: ~5 mg/mL (~8.5 mM; with ultrasonication and warming by heating to 60°C)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (0.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (5.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: 0.5 mg/mL (0.85 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (5.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: 0.5 mg/mL (0.85 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (5.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
