2. Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. Complement System VEGFR
  4. NRPa-308

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.

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NRPa-308

NRPa-308 Chemical Structure

CAS No. : 717863-53-1

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Based on 1 publication(s) in Google Scholar

NRPa-308 Related Antibodies

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Description

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[1].

In Vitro

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.

NRPa-308 Related Antibodies

Cell Migration Assay [1]

Cell Line: Human Umbilical Vein Endothelial Cells (HUVEC), MDA-MB-231 human breast cancer cells
Concentration: 0.2 μM
Incubation Time: 24 h
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.
In Vivo

NRPa-308 (compound 2a) (50 mg/kg; oral gavage; every three days; 20 days) increases median mouse survival by 20%, reduces tumour growth, disrupts tumour angiogenesis, and shows no acute toxicity in a human MDA-MB-231 breast cancer xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 50 mg/kg
Administration: oral gavage; every three days; 20 days
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.
Molecular Weight

424.51

Formula

C23H24N2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C)C(S(=O)(NC2=CC=C(C)C=C2)=O)=C1)NC3=C(OCC)C=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3557 mL 11.7783 mL 23.5566 mL
5 mM 0.4711 mL 2.3557 mL 4.7113 mL
View the 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.

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Purity & Documentation
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
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NRPa-308 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NRPa-308717863-53-1NRPa308NRPa 308Complement SystemVEGFRVascular endothelial growth factor receptorNRP-1human solid cancer cellshuman breast cancer cellshuman haematological cancer cellsHUVECNeuropilin-1mouse xenograft modelsangiogenesisVEGF-A165MDA-MB-231 human breast cancer cellsInhibitorinhibitorinhibit

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