Apatinib Mesylate
(Synonyms: 阿帕替尼) 目录号 : GC14292
A selective VEGFR2 inhibitor
Cas No.:811803-05-1
Sample solution is provided at 25 µL, 10mM.
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.
阿帕替尼阻断 VEGF 通路的下游信号转导，从而抑制新生血管形成。阿帕替尼对肉瘤、乳腺癌、卵巢癌、急性淋巴细胞白血病（ALL）等多种肿瘤均显示出抗肿瘤作用。此外，最近的病例报告为阿帕替尼治疗上皮样恶性多发性间皮瘤提供了支持信息。[1]
体外实验表明，阿帕替尼以剂量依赖性和时间依赖性方式抑制细胞增殖。阿帕替尼作用于MPM细胞24 h、48 h、72 h的IC50值分别为46.34 μM、45.14 μM、28.73 μM。[3]
体内实验表明，阿帕替尼可抑制肿瘤生长和转移。空白对照、溶剂对照和阿帕替尼组的ePCI评分分别为9.8±0.9、10.3±0.9和7.3±1.6。差异具有统计学意义（所有 P = 0.003；P = 0.008，空白对照与阿帕替尼组；P = 0.001，溶剂对照与阿帕替尼组；P = 0.394，空白对照与溶剂对照）。阿帕替尼组Ki-67阳性率为（17.0±8.0）%，显着低于对照组的（48.1±11.5）%（P=0.000）；阿帕替尼组VEGFR-2阳性率略低于对照组，无统计学意义。[1]
| Cell experiment [1]: | |
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Cell lines |
Primary cells established by s.c. tumors |
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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. |
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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. |
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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 [1]: | |
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Animal models |
Specific pathogen free BALB/c nu/nu mice, 4–5 weeks old, 16–18 g |
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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 μg/g/d 0.5% CMC, and treatment group was treated with 100 μg/g/d apatinib delivered by intra-gastric gavage. The treatment process lasted for 2 weeks. |
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Dosage form |
100 μg/g/d; apatinib was diluted in 0.5% Carboxymethyl Cellulose-Na solution |
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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 |
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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. |
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| Cas No. | 811803-05-1 | SDF | |
| 别名 | 阿帕替尼 | ||
| 化学名 | 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 | ||
| 分子式 | C25H27N5O4S | 分子量 | 493.58 |
| 溶解度 | ≥ 49.4mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
VEGFA derived from hypoxic PMCs facilitates GC cell adhesion and migration via VEGFR1. a The effect of exogenous VEGFA on cell migration was observed in the presence of Apatinib or Bevacizumab. Representative photographs of migratory cells are shown. Scale bar represents 100 μm.
Apatinib were obtained from GlpBio.
J Exp Clin Canc Res 39.1 (2020): 1-14. PMID: 33081836 IF: 11.163 -
Related Biological Data
Targeting SMYD2 synergistically increases the antiangiogenic activity of apatinib in CRC.IHC staining revealed that both BAY-598 and apatinib treatment reduced CD31 levels, but more satisfactory effects were achieved when the two treatments were combined.
Then, we treated CRC cells with DMSO, BAY-598, apatinib (10 μM), or BAY-598 (10 μM) combined with apatinib(GLPBIO) for 48 h, and prepared TCM according to the standard method.
Angiogenesis (2022): 1-18. PMID: 35503397 IF: 9.5957 -
Related Biological Data
Art-M improves the antitumor effect of apatinib in GC both in vivo and in vitro. (A) Total number of viable cells was counted after treatment of MGC803 and AGS cells with different concentrations of apatinib for 96 h.
Male nude mice carrying GC xenografts were randomly divided into four groups and given Art-M (2 mg/kg; i.p.; once daily), apatinib(GlpBio) (50 mg/kg; p.o.; once daily), or both for 24 days.
Chem-Biol Interact (2023): 110618. PMID: 37394161 IF: 5.1