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Apatinib Mesylate (Synonyms: YN968D1)

Catalog No.GC14292

Apatinib blocks the downstream signal transduction of VEGF pathway to inhibit neovascularization.

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Apatinib Mesylate Chemical Structure

Cas No.: 811803-05-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$153.00
In stock
5mg
$136.00
In stock
10mg
$158.00
In stock
25mg
$252.00
In stock
50mg
$391.00
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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 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.

Chemical Properties

Cas No. 811803-05-1 SDF
Synonyms 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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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.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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

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