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Apatinib Mesylate (Synonyms: YN968D1)

Catalog No.GC14292

Apatinib bloque la transduction du signal en aval de la voie VEGF pour inhiber la néovascularisation.

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Apatinib Mesylate Chemical Structure

Cas No.: 811803-05-1

Taille Prix Stock Qté
10mM (in 1mL DMSO)
153,00 $US
En stock
5mg
136,00 $US
En stock
10mg
158,00 $US
En stock
25mg
252,00 $US
En stock
50mg
391,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 3 publications

Product Documents

Quality Control & SDS

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Protocol

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.

Background

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.

Chemical Properties

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.

Complete Stock Solution Preparation Table

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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
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Review for Apatinib Mesylate

Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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