Size | Price | Stock | Qty |
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5mg |
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Other Sizes |
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Targets |
VEGFR3 11 nM (IC50) VEGFR1 396 nM (IC50) VEGFR2 130 nM (IC50) ERK 13 nM (IC50)
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ln Vitro |
In HEK293 cells, VEGFR-1/2/3 autophosphorylation is dose-dependently inhibited by EVT801 (10 nM-1 μM), with IC50s of 39 nM (VEGFR-3), 2130 nM (VEGFR-1), and 260 nM (VEGFR-2), respectively[1]. Proliferation of VEGFR-3-positive cells, such as human lymphatic microvascular endothelial cells (hLMVEC), is inhibited by EVT801 (1 nM-1 μM). EVT801 has dose-dependent inhibitory concentrations (IC50s) of 15 nM for VEGF-C, 8 nM for VEGF-D, and 155 nM for VEGF-A that prevent the induction of hLMVECs proliferation[1]. VEGFR-3-positive tumor cells' proliferation and tumor growth are inhibited by EVT801 (1 μM)[1].
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ln Vivo |
EVT801 (30 mg/kg; po; twice daily for 7 d) inhibits tumors that are positive for VEGFR-3 in mouse models, including the RT-001-HAM Subcutaneous Patient-derived xenograft (PDx) Tumor Mouse Model, the 4T1 Mammary Carcinoma Mouse Model, the N-Diethylnitrosamine-Induced Hepatocarcinoma Mouse Model, the NCI-H1703 Subcutaneous Xenograft Tumor Mouse Model, the Rip1-Tag2/transgenic Mouse Models, and the CT26 Ectopic Tumor Mouse Model. In addition to tumor cells found in endothelial malignancies, EVT801 is expressed in blood arteries containing primary tumors and metastases of kidney cancer[1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: VEGFR-3-positive cells, human lymphatic microvascular endothelial cells (hLMVEC) Tested Concentrations: 1 nM-1 μM Incubation Duration: Experimental Results: demonstrated a maximum inhibition of 74%, 100%, and 65% against VEGF -C, VEGF-D, VEGF-A induction, respectively. |
References |
[1]. Paillasse M R, et al. Targeting Tumor Angiogenesis with the Selective VEGFR-3 Inhibitor EVT801 in Combination with Cancer Immunotherapy[J]. Cancer Research Communications, 2022, 2(11): 1504-1519.
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Molecular Formula |
C19H21N5O3
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Molecular Weight |
367.40
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CAS # |
1412453-70-3
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SMILES |
N1(CC)C2C(=CC=C(C#C[C@](O)(C)COC)N=2)C(=O)C(C2NC=CN=2)=C1N
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7218 mL | 13.6091 mL | 27.2183 mL | |
5 mM | 0.5444 mL | 2.7218 mL | 5.4437 mL | |
10 mM | 0.2722 mL | 1.3609 mL | 2.7218 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.