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EG00229

Catalog No. T11153 CAS 1210945-69-9

EG00229 is a neuropilin 1 (NRP1) receptor antagonist that selectively inhibits the binding of VEGF-A to the NRP1 b1 domain, achieving this inhibition with an IC50 value of 3 μM. It does not affect the binding of VEGF-A to other receptors, such as VEGFR-1 and VEGFR-2.

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EG00229, CAS 1210945-69-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
2 mg	In stock	$ 64.00
5 mg	In stock	$ 101.00
10 mg	In stock	$ 159.00
25 mg	In stock	$ 265.00
50 mg	In stock	$ 392.00
100 mg	In stock	$ 583.00
1 mL * 10 mM (in DMSO)	In stock	$ 143.00

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Purity: 97.20%

Biological Description

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Description	EG00229 is a neuropilin 1 (NRP1) receptor antagonist that selectively inhibits the binding of VEGF-A to the NRP1 b1 domain, achieving this inhibition with an IC50 value of 3 μM. It does not affect the binding of VEGF-A to other receptors, such as VEGFR-1 and VEGFR-2.
Targets&IC50	Bt-VEGF-A binding to purified NRP1 b1 domain:3 μM , [125I]-VEGF-A binding to PAE/NRP1:8 μM
In vitro	EG00229 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.EG00229 ( 0-100 μM; 48 hours; A549 cells) treatment causes a significant reduction in cell viability over a 48 hours incubation. EG00229 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.
In vivo	EG00229 treatment substantially reduces tumor growth and visible vascularization.

Molecular Weight	611.6
Formula	C19H20F3N7O7S3
CAS No.	1210945-69-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 41.4 mg/mL (67.69 mM)

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

EG00229 1210945-69-9 Others EG 00229 EG-00229 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.