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Apatinib Mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Apatinib Mesylate图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍

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 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

文献引用
产品描述

Apatinib blocks the downstream signal transduction of VEGF pathway to inhibit neovascularization. Apatinib has showed antitumor effects on many kinds of tumors, such as sarcoma, breast cancer, ovarian cancer, and acute lymphoblastic leukemia (ALL). Moreover, a recent case report provided supporting information for apatinib to treat epithelioid malignant plural mesothelioma.[1]

In vitro experiment indicated that apatinib inhibited cells proliferation in a dose-dependent and time-dependent manner. The IC50 values of apatinib in MPM cells for treatment time 24 h, 48 h, 72 h were 46.34 μM, 45.14 μM, 28.73 μM.[3]

In vivo experiments demonstrated that apatinib inhibits tumor growth and metastasis. The ePCI score of blank control, solvent control and apatinib groups were 9.8 ± 0.9, 10.3 ± 0.9, and 7.3 ± 1.6, respectively. The differences were statistically significant (P = 0.003 for all; P = 0.008, blank control vs. apatinib group; P = 0.001, solvent control vs. apatinib group; P = 0.394, blank control vs. solvent control). The positive rate of Ki-67 in apatinib group was (17.0 ± 8.0)%, which is significantly lower than that in control group (48.1 ±11.5) % (P = 0.000); the positive rate of VEGFR-2 in apatinib group was slightly lower than that in control group, indicating no statistical significance.[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.