Tivozanib (AV-951) |
| カタログ番号GC12036 |
チボザニブ (AV-951; KRN951) は、VEGFR-1、VEGFR-2、VEGFR-3 の IC50 がそれぞれ 0.21、0.16、0.24 nM である、強力かつ選択的で経口的に活性な VEGFR チロシンキナーゼ阻害剤です。チボザニブは、腫瘍組織の血管新生と血管透過性を阻害し、抗腫瘍活性を示します。チボザニブは、転移性腎細胞癌 (RCC) の研究の可能性を秘めています。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 475108-18-0
Sample solution is provided at 25 µL, 10mM.
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Product Documents
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Protocol
| Cell experiment [1]: | |
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Cell lines |
Human ovarian carcinoma cell lines, including A2780CP, OVCAR3 and SKOV3. |
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Preparation method |
Soluble in DMSO >22.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
10μm, 48h |
|
Applications |
Combination of tivozanib with the EGFR(Epidermal Growth Factor Receptor)-directed therapies displayed synergistic activity on cell growth inhibition and induction of apoptosis, suggesting that anti-VEGFR(vascular endothelial growth factor receptor) -targeted approaches induced sensitisation to the EGFR-directed therapies. |
| Clinical experiment [2]: | |
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Diseases models |
Patients with renal cell carcinoma(RCC) |
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Dosage form |
1.5 mg OD for 3 weeks, oral administration |
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Application |
Tivozanib exhibit an inhibitory profile with high sensitivity for inhibition of VEGFR family members. Patients receiving tivozanib had a PFS(Progression free survival) of 12.7 months – the best PFS reported in a phase III trial with mRCC. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Momeny M1, Sabourinejad Z2,3, et al, Anti-tumour activity of tivozanib, a pan-inhibitor of VEGF receptors, in therapy-resistant ovarian carcinoma cells. Sci Rep. 2017 Apr 6;7:45954. doi: 10.1038/srep45954. [2]. Grünwald V1, Merseburger AS2. The progression free survival-plateau with vascular endothelial growth factor receptor inhibitors – Is there more to come Eur J Cancer. 2013 Jul;49(11):2504-11. doi: 10.1016/j.ejca.2013.03.022. Epub 2013 Apr 16. |
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| Cas No. | 475108-18-0 | SDF | |
| Chemical Name | 1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea | ||
| Canonical SMILES | CC1=CC(=NO1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)Cl | ||
| Formula | C22H19ClN4O5 | M.Wt | 454.86 |
| 溶解度 | ≥ 22.75mg/mL in DMSO | 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. | ||
Complete Stock Solution Preparation Table
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1985 mL | 10.9924 mL | 21.9848 mL |
| 5 mM | 0.4397 mL | 2.1985 mL | 4.397 mL |
| 10 mM | 0.2198 mL | 1.0992 mL | 2.1985 mL |
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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.
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レビュー
Average Rating: 5 ★★★★★ (Based on Reviews and 32 reference(s) in Google Scholar.)
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