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EG01377 2HCl

Catalog No. T11154L CAS 2749438-61-5

Synonyms: EG01377 2HCl(2227996-00-9 Free base)

EG01377 2HCl is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1) with a Kd value of 1.32 μM and an IC50 value of 609 nM for both EG01377 2HCl against NRP1-a1 and NRP1-b1.EG01377 exhibits anti-angiogenic, antimigratory and antitumor activities.

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EG01377 2HCl, CAS 2749438-61-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 148.00
5 mg	In stock	$ 372.00
10 mg	In stock	$ 568.00
25 mg	In stock	$ 915.00
50 mg	In stock	$ 1,250.00
100 mg	In stock	$ 1,680.00
500 mg	In stock	$ 3,370.00
1 mL * 10 mM (in DMSO)	In stock	$ 539.00

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Purity: 99.56%

ee: 100%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	EG01377 2HCl is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1) with a Kd value of 1.32 μM and an IC50 value of 609 nM for both EG01377 2HCl against NRP1-a1 and NRP1-b1.EG01377 exhibits anti-angiogenic, antimigratory and antitumor activities.
Targets&IC50	NRP1-a1 and NRP1-b:609 nM
In vitro	EG0 1377 2HCl (30 μM) effectively diminishes HUVEC cell migration induced by VEGFA. Additionally, EG01377 2HCl leads to reductions in network area, length, and branching points.[1] EG0 1377 2HCl (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC50 of 30 μM.[1] EG0 1377 2HCl (30 μM; 5 days) can delay the VEGF-induced wound closure.[1] EG0 1377 2HCl diminishes VEGF-triggered angiogenesis. Moreover, when combined with VEGFA, EG01377 2HCl curtails spheroid outgrowth of A375P (malignant melanoma) cells.[1] EG0 1377 2HCl (500 nM; 2 h) blocks the production of transforming growth factor beta (TGFβ) by Nrp1+ regulatory T-cell SMAD3/AKT (Tregs) in the presence of tumor cell-derived factors.[1]
In vivo	EG0 1377 2HCl (2 mg/kg; i.v.; BABL/c female mice) possesses a half-life of 4.29 hours, allowing for once-a-day dosing to be maintained in mice.[1]

Synonyms	EG01377 2HCl(2227996-00-9 Free base)
Molecular Weight	659.6
Formula	C26H32Cl2N6O6S2
CAS No.	2749438-61-5

Storage

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

Solubility Information

DMSO: 180.0 mg/mL (272.9 mM), Sonication is recommended.

References and Literature

1. Powell J, et al. Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells. J Med Chem. 2018;61(9):4135-4154. 2. Klaewkla M, et al. Molecular basis of the new COVID-19 target neuropilin-1 in complex with SARS-CoV-2 S1 C-end rule peptide and small-molecule antagonists. J Mol Liq. 2021;335:116537. 3. Zhang P, et al. NRP1 promotes prostate cancer progression via modulating EGFR-dependent AKT pathway activation. Cell Death Dis. 2023;14(2):159.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Bioactive Compound Library

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Keywords

EG01377 2HCl 2749438-61-5 Immunology/Inflammation Complement System EG01377 2HCl(2227996-00-9 Free base) EG-01377 EG01377 EG 01377 inhibitor inhibit

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