NRPa-308
Based on 1 Customer Validation
NRPa-308 is a potent and orally active Neuropilin-1 (NRP-1) antagonist with an IC50 of 42 μM for inhibiting VEGF-A165 binding to NRP-1. NRPa-308 blocks the specific interaction between VEGF-A165 and NRP-1. NRPa-308 effectively suppresses angiogenesis in vitro and in vivo and reduces the viability of a broad spectrum of human solid and haematological cancer cells. NRPa-308 inhibits tumor growth and prolongs median survival in a human breast cancer xenograft mouse model. NRPa-308 can be used for the research of multiple human malignancies including solid tumors and hematological cancers.
For research use only. We do not sell to patients.
- Purity: 98.96%
- CAS No.: 717863-53-1
- Formula: C23H24N2O4S
- Molecular Weight:424.51
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All VEGFR Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-549 | IC50 |
0.1 μM
Compound: 1; NRPa-308
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Antiproliferative activity against human BT549 cells expressing NRP1 assessed as cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human BT549 cells expressing NRP1 assessed as cell viability measured after 72 hrs by MTT assay
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[PMID: 31699610] |
NRPa-308 (compound 2a) (10-42 μM; 1-2 h) inhibits VEGF-A165 binding to purified NRP-1 protein with an IC50 of 42 μM, and achieves 32% inhibition at a concentration of 10 μM[1].
NRPa-308 (0.2 μM; 72 h) reduces adhesion of HUVEC with an IC50 of 0.2 μM[1].
NRPa-308 (72 h) inhibits adhesion and viability of HUVEC (IC50 = 0.2 μM) as well as adhesion of MDA-MB-231 human breast cancer cells (IC50 = 0.5 μM)[1].
NRPa-308 (72 h) reduces viability of native, Shcontrol-modified, and ShVEGF-R2-modified MDA-MB-231 human breast cancer cells with IC50 values of 0.6 μM, 0.8 μM, and 0.9 μM respectively, but loses potency (IC50 = 9.0 μM) on ShNRP-1-modified MDA-MB-231 cells following 72 h of treatment[1].
NRPa-308 (24-72 h) reduces viability of most tested human solid and haematological cancer cell lines with IC50 values ranging from 0.10 μM to 0.60 μM after 72 h treatment, shows weaker potency against normal human fibroblasts and lymphatic endothelial cells (IC50 = 20.8 μM and 11.2 μM respectively), and exhibits no effect (IC50 ≥ 10 μM) on select solid and haematological cancer cell lines[1].
NRPa-308 (0.2 μM; 24 h) dramatically inhibits tubule formation and significantly reduces the migratory speed of VEGF-A165-stimulated HUVEC and MDA-MB-231 human breast cancer cells following 24 h of incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human Umbilical Vein Endothelial Cells (HUVEC), MDA-MB-231 human breast cancer cells
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Concentration:0.2 μM
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Incubation Time:24 h
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Result:Reduced HUVEC migratory speed to 55 pixels/h after 24 h.
Reduced MDA-MB-231 migratory speed to 5.23 μm/h after 24 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/scid/IL-2Rγ-/- (NOG) (female, 6-7 weeks old, subcutaneous injection of 2×106 human MDA-MB-231 breast cancer cells)[1]
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Dosage:50 mg/kg
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Administration:oral gavage; every three days; 20 days
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Result:Increased median survival by 20% (from 35 to 42 days post-xenograft).
Reduced tumour growth.
Disrupted the tumour vessel network.
Caused no visible weight loss or acute toxicity.
Detected no metastases in treated mice euthanized at day 46 post-xenograft.
Chemical Information
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CAS No. 717863-53-1
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Appearance Solid
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Molecular Weight 424.51
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Formula C23H24N2O4S
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Color White to off-white
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SMILES
O=C(C1=CC=C(C)C(S(=O)(NC2=CC=C(C)C=C2)=O)=C1)NC3=C(OCC)C=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (235.57 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. 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. 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)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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. 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 | 2.3557 mL | 11.7783 mL | 23.5566 mL | 58.8914 mL |
| 5 mM | 0.4711 mL | 2.3557 mL | 4.7113 mL | 11.7783 mL | |
| 10 mM | 0.2356 mL | 1.1778 mL | 2.3557 mL | 5.8891 mL | |
| 15 mM | 0.1570 mL | 0.7852 mL | 1.5704 mL | 3.9261 mL | |
| 20 mM | 0.1178 mL | 0.5889 mL | 1.1778 mL | 2.9446 mL | |
| 25 mM | 0.0942 mL | 0.4711 mL | 0.9423 mL | 2.3557 mL | |
| 30 mM | 0.0785 mL | 0.3926 mL | 0.7852 mL | 1.9630 mL | |
| 40 mM | 0.0589 mL | 0.2945 mL | 0.5889 mL | 1.4723 mL | |
| 50 mM | 0.0471 mL | 0.2356 mL | 0.4711 mL | 1.1778 mL | |
| 60 mM | 0.0393 mL | 0.1963 mL | 0.3926 mL | 0.9815 mL | |
| 80 mM | 0.0294 mL | 0.1472 mL | 0.2945 mL | 0.7361 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5889 mL |