hVEGF-IN-1 |
| カタログ番号GC32963 |
キナゾリン誘導体であるhVEGF-IN-1は、内部リボソーム侵入部位A（IRES-A）のGリッチ配列に特異的に結合し、G四重鎖構造を不安定化する可能性があります。 ｈＶＥＧＦ－ＩＮ－１は、ＳＰＲ実験において０．９２８μＭのＫｄでＩＲＥＳ－Ａ（ＷＴ）に結合する。 hVEGF-IN-1 は、VEGF-A タンパク質の発現を減少させることにより、腫瘍細胞の移動を妨げ、腫瘍の成長を抑制する可能性があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1637443-98-1
Sample solution is provided at 25 µL, 10mM.
hVEGF-IN-1 represses human VEGF-A translation and shows antitumor activity.
hVEGF-IN-1 shows a significant specific interaction with the G-rich region within the 5′- untranslated regions (5′-UTR) of hVEGF-A mRNA and destabilizes the Gquadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM and binds to the hairpin DNA with a Kd of 21.2 μM. The G-rich sequence G774-G790 within the IRES-A of hVEGF-A's 5′-UTR has been shown to be critical for the translation initiation activity of IRES-A. hVEGF-IN-1 hinders BG4 from binding to the IRES-A RNA G-quadruplex in cells. hVEGF-IN-1 down-regulates hVEGF-A's translation via the G-quadruplex within IRES-A mRNA. hVEGF-IN-1 treatment reduces MDA-MB- 231 cell migration to approximately 25%[1].
Tumor bearing mice treated with hVEGF-IN-1 have an average tumor volume of less than 300 mm3. The tumor weight in the presence of hVEGF-IN-1 reduces around 60.1% to a final weight of 0.18 g. No significant change in body weight is observed during the treatment[1].
[1]. Discovery of Small Molecules for Repressing Cap-Independent Translation of Human VascularEndothelial Growth Factor (hVEGF) as Novel Antitumor Agents. J Med Chem. 2017 Jul 13;60(13):5306-5319.
Cell experiment: | MDA-MB-231 cells are plated in the top chambers of 0.8 μm pore trans-wells in Opti-MEM reduced serum medium in the presence or absence of hVEGF-IN-1. Meanwhile, 600 μL of DMEM containing 10% fetal bovine serum (FBS) and 100 μM CoCl2 are added to the lower chambers. The cells are allowed to migrate for 24 h. At the end of the assay, the cells in the top chamber are removed, and the cells at the bottom of the filter are treated by adding 500 μL of DMEM containing 2.5 mg/mL MTT to each well. After incubating at 37 °C with 5% CO2 for 4 h, 500 μL of DMSO is added to each well and the plate is gently rotated for 10 min. Absorbance (570 nm) is measured using a microplate reader[1]. |
Animal experiment: | Mice: Mice are separated into three groups: negative control, compound 1-treated, and positive control (doxorubicin-treated). hVEGF-IN-1, doxorubicin, and saline are administered by ip injection to athymic nude mice with human tumor xenografts established using MCF-7 breast cancer cells. Mice are injected ip once a day for 20 days. Negative controls are injected with 150 μL of saline. The positive control group received doxorubicin by ip injection at a dose of 1 mg/kg. hVEGF-IN-1 is similarly administered to mice at a dose of 7.5 mg/kg. After treating the animals for 20 days, the tumor tissues are collected and IHC assays are conducted using an anti-VEGF-A antibody[1]. |
References: [1]. Discovery of Small Molecules for Repressing Cap-Independent Translation of Human VascularEndothelial Growth Factor (hVEGF) as Novel Antitumor Agents. J Med Chem. 2017 Jul 13;60(13):5306-5319. | |
| Cas No. | 1637443-98-1 | SDF | |
| Canonical SMILES | CCN(CC)CCOC(C=C1)=CC=C1NC2=NC(C3=C(NC(CCN4CCN(C)CC4)=O)C=CC=C3)=NC5=CC=CC=C52 | ||
| Formula | C34H43N7O2 | M.Wt | 581.75 |
| 溶解度 | DMSO : 25 mg/mL (42.97 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.719 mL | 8.5948 mL | 17.1895 mL |
| 5 mM | 0.3438 mL | 1.719 mL | 3.4379 mL |
| 10 mM | 0.1719 mL | 0.8595 mL | 1.719 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *