Apatinib Mesylate (Synonyms: YN968D1) |
Catalog No.GC14292 |
Apatinib bloque la transduction du signal en aval de la voie VEGF pour inhiber la néovascularisation.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 811803-05-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
Primary cells established by s.c. tumors |
Preparation Method |
Apatinib was dissolved in DMSO to yield a 151 mM stock solution, which was then diluted to the specified concentration in subsequent experiment by using DMEM. |
Reaction Conditions |
Cells were treated with different concentrations of apatinib (0, 12.5, 25, 50 and 100 mM) for 24, 48, and 72 h, respectively. |
Applications |
This could be used to test the ability of apatinib on the inhibitions of MPM Cells’ viability and proliferation. These gradient concentrations of apatinib inhibited cells proliferation; the inhibitory effect of apatinib on MPM cells showed the dose-dependent and time-dependent manner. |
Animal experiment [2]: | |
Animal models |
Specific pathogen free BALB/c nu/nu mice, 4–5 weeks old, 16–18 g |
Preparation Method |
MPM surgical specimens was made to establish patient-derived xenograft (PDX) models in nude mice. Eighteen nude mice were randomly divided into three groups: blank control, solvent control and apatinib groups. Blank control group received no intervention, solvent control group was administrated with 24 mg/g/day 0.5% CMC, and treatment group was treated with 100 mg/g/day apatinib delivered by intra-gastric gavage. The treatment process lasted for 2 weeks. |
Dosage form |
100 mg/g/day; apatinib was diluted in 0.5% Carboxymethyl Cellulose-Na solution |
Applications |
This could be used to test the efficacy and toxicity of apatinib on MPM PDX Model. Results indicated that apatinib did not affect the weight of nude mice, and no adverse effects were observed during the construction of mice models. The positive rate of Ki-67 in apatinib group is significantly lower than that in control group |
References: [1]. Yang ZR, et al. Apatinib Mesylate Inhibits the Proliferation and Metastasis of Epithelioid Malignant Peritoneal Mesothelioma In Vitro and In Vivo. Front Oncol. 2020 Dec 7;10:585079. |
Apatinib bloque la transduction du signal en aval de la voie VEGF pour inhiber la néovascularisation. Apatinib a montré des effets antitumoraux sur de nombreux types de tumeurs, telles que le sarcome, le cancer du sein, le cancer de l'ovaire et la leucémie lymphoblastique aiguë (LLA). De plus, un récent rapport de cas a fourni des informations favorables à l'utilisation d'apatinib dans le traitement du mésothéliome pleural malin épithélioïde.[1]
L'expérience in vitro a indiqué que l'apatinib inhibait la prolifération des cellules de manière dose-dépendante et temps-dépendante. Les valeurs IC50 de l'apatinib dans les cellules MPM pour un temps de traitement de 24 h, 48 h, 72 h étaient respectivement de 46,34 μM, 45,14 μM et 28,73 μM.[3]
Des expériences in vivo ont démontré que l'apatinib inhibe la croissance tumorale et les métastases. Le score ePCI des groupes de contrôle vierge, de contrôle de solvant et d'apatinib étaient respectivement de 9,8 ± 0,9, 10,3 ± 0,9 et 7,3 ± 1,6. Les différences étaient statistiquement significatives (P = 0,003 pour tous ; P = 0,008 pour le groupe témoin vierge vs. le groupe apatinib ; P = 0,001 pour le groupe témoin de solvant vs. le groupe apatinib ; P = 0 ,394 pour le groupe témoin vierge vs. le groupe témoin de solvant). Le taux positif de Ki-67 dans le groupe apatinib était (17.0 ±8.0) % ce qui est significativement plus faible que celui du groupe témoin (48.1±11.5)% (P=0.000); Le taux positif du VEGFR-2 dans le groupe apatinib était légèrement inférieur à celui du groupe témoin indiquant qu'il n'y avait pas une signification statistique.[1]
References:
[1]. Yang ZR, et al. Apatinib Mesylate Inhibits the Proliferation and Metastasis of Epithelioid Malignant Peritoneal Mesothelioma In Vitro and In Vivo. Front Oncol. 2020 Dec 7;10:585079.
Cas No. | 811803-05-1 | SDF | |
Synonymes | YN968D1 | ||
Chemical Name | N-[4-(1-cyanocyclopentyl)phenyl]-2-(pyridin-4-ylmethylamino)pyridine-3-carboxamide;methanesulfonic acid | ||
Canonical SMILES | CS(=O)(=O)O.C1CCC(C1)(C#N)C2=CC=C(C=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4 | ||
Formula | C25H27N5O4S | M.Wt | 493.58 |
Solubility | ≥ 49.4mg/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. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.026 mL | 10.1301 mL | 20.2601 mL |
5 mM | 0.4052 mL | 2.026 mL | 4.052 mL |
10 mM | 0.2026 mL | 1.013 mL | 2.026 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.
Average Rating: 5
(Based on Reviews and 39 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 *