| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
VEGFR2-IN-84 (E20) (4.92 nM; 96 h) significantly inhibited VEGF-induced HUVEC cell proliferation, with an activity approximately 10 times that of lenvatinib [1]. VEGFR2-IN-84 (10-1000 nM; 48 h) dose-dependently inhibited the phosphorylation of VEGFR2 and its downstream molecules AKT and ERK in HUVEC, A549, and HepG2 cells, with activity superior to lenvatinib [1]. VEGFR2-IN-84 (8.53-14.1 μM; 72 h) showed weak inhibitory activity against normal cells LO2, HEK293T, and BEAS-2B, exhibiting good tumor cell selectivity [1].
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| ln Vivo |
VEGFR2-IN-84 (E20) (50 mg/kg; orally; once daily; 21 days) significantly inhibited tumor growth in a male BALB/c nude mouse HepG2 hepatocellular carcinoma xenograft model, with efficacy superior to the same dose of lenvatinib, and did not cause significant weight loss [1]. VEGFR2-IN-84 (30-60 mg/kg; orally; once daily; 20-30 days) dose-dependently inhibited tumor growth in male BALB/c nude mouse A549 lung cancer, 786-O renal cell carcinoma, and 8305C thyroid cancer xenograft models, with efficacy superior to the same dose of lenvatinib [1]. VEGFR2-IN-84 (2 mg/kg; tail vein injection; single dose; 24 hours) showed moderate elimination half-life (T1/2 = 5.05 hours) and plasma exposure (AUC0-∞ = 1970 ng·h/mL) in healthy ICR mice [1].
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| Animal Protocol |
Animal/Disease Models:Male BALB/c nude mice (4-5 weeks old, 15-17 g), HepG2 hepatocellular carcinoma subcutaneous xenograft model [1]
Doses: 50 mg/kg Route of Administration:Oral gavage (po), once daily (qd) Experimental Results:Significantly inhibited the growth of HepG2 xenograft tumors, with a tumor growth inhibition rate (TGI) of 94.3%, which was superior to lenvatinib at the same dose (TGI=83.6%). No significant weight loss or significant toxicity was observed throughout the experiment. Animal/Disease Models:Male BALB/c nude mice (4-5 weeks old, 15-17 g), A549 non-small cell lung cancer subcutaneous xenograft model [1] Doses: 30 mg/kg or 60 mg/kg Route of Administration: Oral gavage (po), once daily (qd) Experimental Results: Showed dose-dependent antitumor activity. At a dose of 30 mg/kg, the tumor growth inhibition rate (TGI) was 76.9%, which was superior to lenvatinib at the same dose (TGI=61.3%). At a dose of 60 mg/kg, the TGI reached 95.7%, which was significantly superior to lenvatinib (TGI=84.6%). No significant weight loss was observed. |
| References |
| Molecular Formula |
C25H18N4O4S
|
|---|---|
| Molecular Weight |
470.50
|
| CAS # |
861877-12-5
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
NC(C1=C(C=C(C2=C1)N=CC=C2OC3=CC4=C(C=C3)C(C(NC5=NC=CS5)=O)=CC=C4)OC)=O
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| HS Tariff Code |
2934.99.9001
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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 Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1254 mL | 10.6270 mL | 21.2540 mL | |
| 5 mM | 0.4251 mL | 2.1254 mL | 4.2508 mL | |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1254 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.
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