EG00229 trifluoroacetate
Based on 12 publication(s) in Google Scholar
EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.03%
- CAS No.: 1210945-69-9
- 화학식: C19H20F3N7O7S3
- 분자량:611.60
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) EG00229 trifluoroacetate
More- EBioMedicine. 2019 May:43:525-536. [Abstract]
- Proc Natl Acad Sci U S A. 2026 Mar 31;123(13):e2510265123. [Abstract]
- Acta Pharmacol Sin. 2026 Feb 19. [Abstract]
- Mol Med. 2025 Dec 16;31(1):336. [Abstract]
- Fluids Barriers CNS. 2024 Apr 8;21(1):32. [Abstract]
- Biochem Pharmacol. 2026 Jun 12;251(Pt 2):118163. [Abstract]
- Biochem Pharmacol. 2025 Jul 18:241:117183. [Abstract]
- Biochem Pharmacol. 2022 May;199:115030. [Abstract]
- J Cancer. 2021 Aug 24;12(20):6105-6117. [Abstract]
- Bioorg Med Chem. 2020 Jan 1;28(1):115183. [Abstract]
- Cell Physiol Biochem. 2017;44(3):1251-1262. [Abstract]
- bioRxiv. 2024 Oct 21:2023.12.06.570398. [Abstract]
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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RT-PCR
Biological Activity
IC50: 8 μM (125I-VEGF-A binding to PAE/NRP1); 3 μM (bt-VEGF-A binding to purified NRP1 b1 domain)[1].
EG00229 (Compound 2; 0-100 μM; 48 hours; A549 cells) treatment causes a significant reduction in cell viability over a 48 hours incubation[1].
EG00229 (Compound 2) demonstrates inhibition of VEGF-A binding to NRP1 and attenuates VEGFR2 phosphorylation in endothelial cells. Inhibition of migration of endothelial cells is also observed in HUVECs[1].
EG00229 (Compound 2) selectively inhibits radiolabeled 125I-VEGF-A binding to porcine aortic endothelial (PAE)/NRP1, but not VEGFR2-expressing cells, with an IC50 of 8 μM. EG00229 also inhibits VEGF-A binding to lung carcinoma A549 and prostate carcinoma DU145 cells, which express NRP1, but not VEGFR1 and VEGFR2, with similar potency. Binding of VEGF-A to human umbilical vein endothelial cells (HUVECs), which express VEGFR2, VEGFR1, and NRP1, is also inhibited by EG00229 with an IC50 of 23 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:0 µM, 10 μM, 30 μM, 100 μM
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Incubation Time:48 hours
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Result:Caused a significant reduction in cell viability.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week old female NOD scid IL2 receptor gamma chain knockout mice (NSG mice) with ECS cells[2]
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Dosage:0 mg/kg, 10 mg/kg
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Administration:Intraperitoneal injection; three times per week; for 4 weeks
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Result:Reduces tumor growth and visible vascularization.
Chemical Information
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CAS No. 1210945-69-9
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Appearance Solid
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분자량 611.60
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화학식 C19H20F3N7O7S3
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Color Light yellow to yellow
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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.O=C(O)C(F)(F)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (12)
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Journal Impact Factor
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Most Recent
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EBioMedicine
Neuropilin-1 aggravates liver cirrhosis by promoting angiogenesis via VEGFR2-dependent PI3K/Akt pathway in hepatic sinusoidal endothelial cells. [Abstract]2019 May:43:525-536. PMID: 31060904
EG00229 trifluoroacetate purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 May:43:525-536. [Abstract]
EG00229 trifluoroacetate (NRP-1 inhibitor) (10-50 μM; once daily for 7 d) concentration-dependently increased the survival rate of fibrotic liver tissues from patients.
EG00229 trifluoroacetate purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 May:43:525-536. [Abstract]
EG00229 trifluoroacetate (NRP-1 inhibitor) (10-50 μM; once daily for 7 d) significantly decreased the mRNA levels of CD31, α-SMA, collagen1α I, and FN in fibrotic liver tissues from patients.
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Proc Natl Acad Sci U S A
Targeting the ANGPTL4/NRP1/ABL1/RAD51 axis reverses cisplatin resistance by impairing DNA damage repair in head and neck cancer. [Abstract]2026 Mar 31;123(13):e2510265123. PMID: 41886374
EG00229 trifluoroacetate purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2026 Mar 31;123(13):e2510265123. [Abstract]
NRP1 inhibitor EG00229 (10-100 μM) blocked ANGPTL4-induced RAD51 phosphorylation in Tyr315 and Tyr54 of NOKSI cells.
EG00229 trifluoroacetate purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2026 Mar 31;123(13):e2510265123. [Abstract]
EG00229 trifluoroacetate (NRPi) (10-50 µM; 48 h) led to an increase in the DDR in CAL27 cells.
EG00229 trifluoroacetate purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2026 Mar 31;123(13):e2510265123. [Abstract]
EG00229 trifluoroacetate (NRPi) (10 mg/kg; i.p.) sensitized CAL27 xenografts mice to a subtherapeutic dose of cisplatin (5 mg/kg) markedly reducing tumor volume respectively.
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Acta Pharmacol Sin
Epigenetic regulation of NDGA and its synergistic inhibition with EZH2 inhibitors in prostate cancer via NRP1. [Abstract]2026 Feb 19. PMID: 41714725 -
Mol Med
Epigenetic reprogramming drives endothelial dysfunction via neuropilin-1 in pulmonary hypertension. [Abstract]2025 Dec 16;31(1):336. PMID: 41402732 -
Fluids Barriers CNS
SARS-CoV-2 causes dysfunction in human iPSC-derived brain microvascular endothelial cells potentially by modulating the Wnt signaling pathway. [Abstract]2024 Apr 8;21(1):32. PMID: 38584257 -
Biochem Pharmacol
Targeting neuropilin-1 attenuates 4-hydroxytamoxifen-induced stemness and sensitizes ERα-re-expressing TNBC to tamoxifen. [Abstract]2026 Jun 12;251(Pt 2):118163. PMID: 42285368 -
Biochem Pharmacol
Pitavastatin overcomes multi-drug resistance in CRC and NSCLC by targeting the NRP1-ZFX axis. [Abstract]2025 Jul 18:241:117183. PMID: 40684995 -
Biochem Pharmacol
Tuftsin ameliorates splenic inflammatory injury by promoting neuropilin-1 in severe acute pancreatitis. [Abstract]2022 May;199:115030. PMID: 35381211 -
J Cancer
2021 Aug 24;12(20):6105-6117. PMID: 34539883 -
Bioorg Med Chem
Discovery of novel nonpeptide small-molecule NRP1 antagonists: Virtual screening, molecular simulation and structural modification. [Abstract]2020 Jan 1;28(1):115183. PMID: 31744780 -
Cell Physiol Biochem
VEGF-A/Neuropilin 1 Pathway Confers Cancer Stemness via Activating Wnt/β-Catenin Axis in Breast Cancer Cells. [Abstract]2017;44(3):1251-1262. PMID: 29179185
EG00229 trifluoroacetate purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2017;44(3):1251-1262. [Abstract]
The inhibitor of NRP-1 called EG00229 decreases sphere and clone formation in MDA-MB-231 cells.
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bioRxiv
2024 Oct 21:2023.12.06.570398. PMID: 38106002
용액&용해도
DMSO : ≥ 41.4 mg/mL (67.69 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 25 mg/mL (40.88 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (280 KB)
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SDS (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6351 mL | 8.1753 mL | 16.3506 mL | 40.8764 mL |
| 5 mM | 0.3270 mL | 1.6351 mL | 3.2701 mL | 8.1753 mL | |
| 10 mM | 0.1635 mL | 0.8175 mL | 1.6351 mL | 4.0876 mL | |
| 15 mM | 0.1090 mL | 0.5450 mL | 1.0900 mL | 2.7251 mL | |
| 20 mM | 0.0818 mL | 0.4088 mL | 0.8175 mL | 2.0438 mL | |
| 25 mM | 0.0654 mL | 0.3270 mL | 0.6540 mL | 1.6351 mL | |
| 30 mM | 0.0545 mL | 0.2725 mL | 0.5450 mL | 1.3625 mL | |
| 40 mM | 0.0409 mL | 0.2044 mL | 0.4088 mL | 1.0219 mL | |
| 50 mM | 0.0327 mL | 0.1635 mL | 0.3270 mL | 0.8175 mL | |
| 60 mM | 0.0273 mL | 0.1363 mL | 0.2725 mL | 0.6813 mL |
EG00229 trifluoroacetate Related Classifications
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