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受注：045-509-1970 |
技術サポート：[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
化学情報
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Synonyms | YN968D1, Rivoceranib | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C25H27N5O4S |
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| 分子量 | 493.58 | CAS No. | 1218779-75-9 | |
| Solubility (25°C)* | 体外 | DMSO | 22 mg/mL (44.57 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Apatinib mesylate (YN968D1, Rivoceranib) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib mesylate induces both autophagy and apoptosis. |
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| in vitro | Apatinib (YN968D1) is a novel, orally bioavailable, selective inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits VEGFR2. Apatinib can also potently suppress the activities of Ret, c-kit and c-src with IC50 of 0.013 μM, 0.429 μM and 0.53 μM, respectively. Apatinib inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. Apatinib significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50 = 0.17μM). Apatinib effectively inhibits proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring. [1] Apatinib reverses ABCB1- and ABCG2-mediated MDR by inhibiting their transport function, but not by blocking the AKT or ERK1/2 pathway or downregulating ABCB1 or ABCG2 expression. Apatinib significantly potentiates the cytotoxicity of established ABCB1 and ABCG2 substrates and increased the accumulation of DOX and Rho 123 in ABCB1- or ABCG2-overexpressing cells. Furthermore, apatinib significantly inhibited the photoaffinity labeling of both ABCB1 and ABCG2 with [125I]iodoarylazidoprazosin in a concentration-dependent manner. [2] |
| in vivo | Apatinib inhibits the growth of a broad range of human tumor xenografts in a significant dose-dependent manner. [1] Apatinib reverses ABCB1-mediated MDR in the nude mouse xenograft model. [2] Apatinib significantly enhances the antitumor activity of doxorubicin in nude mice bearing K562/ADR xenografts. [3] |
| 特徴 | Good anti-tumor effects for gastric and colorectal cancer compared with sorafenib and sunitinib. |
プロトコル(参考用のみ)
| キナーゼアッセイ | Enzyme-linked immunosorbent assay | |
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| A poly(glu, ala, tyr) 6:3:1 random copolymer is used as a tyrosine containing substrate solution. The substrate is stored as a 1 mg/mL stock in PBS at −20 °C and diluted 1 in 500 with PBS in order to coat 96 well plates (100 μL/well). Plates are coated on the day prior to assay, sealed with adhesive seals, and stored overnight at 4 °C. On the day of the assay, the substrate solution is discarded and the assay plate wells are washed once with PBST (PBS containing 0.05% v/v Tween 20) and once with Hepes buffer (50 mM, pH 7.4).Test compounds are diluted with 10% dimethylsulfoxide (DMSO) de-ionized water and 25 μL volumes transferred to wells in the washed assay plates. Manganese chloride solution (40 mM) containing 8 μM ATP is then added (25 μL) to all test wells. Control and blank wells, containing compound diluent and manganese chloride solution with and without ATP, respectively, are also included to determine the dynamic range of the assay. Freshly diluted enzyme (50 μL) is added to each well, and the plates incubated at room temperature for 20 min. The liquid is then discarded and the wells are washed twice with PBST. Mouse IgG anti-phosphotyrosine antibody diluted 1:6000 with PBST containing 0.5% (w/v) bovine serum albumin (BSA) is added (100 μL/well), and the plates incubated for 1h at room temperature before discarding the liquid and washing the wells twice with PBST. Horseradish peroxidase (HRP)-linked sheep anti-mouse Ig antibody diluted 1:500 with PBST containing 0.5% (w/v) BSA, is then added (100 μL/well) and the plates incubated for a further 1 h at room temperature before discarding the liquid and washing the wells twice with PBST. A 1 mg/mL solution of 2,2‘-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid is freshly prepared in 50 mM phosphate-citrate buffer (pH5.0) containing 0.03% (w/v) sodium perborate, and 100 μL added to each well. Plates are then incubated for 20−60 min at room temperature until the optical density value of control wells measured at 405 nm is approximately 1.0. IC50 values for compound enzyme inhibition are interpolated using Microcal Origin following subtraction of blank values. | ||
| 細胞アッセイ | 細胞株 | HUVEC |
| 濃度 | ~25 μM | |
| 反応時間 | 72 h | |
| 実験の流れ | The HUVEC are seeded into 96-well plates. After 24 h of incubation, cells are exposed to the test agents (vehicle as control) together with 20 ng/mL VEGF or 20% FBS for another 72 h. After fixation with 10% trichloroacetic acid, the cells are stained with 0.4% sulforhodamine B for 30 min at 37 °C and then washed with 1% acetic acid. Tris is added to dissolve the complex, and the optical density is measured at 520 n |
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| 動物実験 | 動物モデル | Ls174t, HCT 116, SGC-7901, HT-29, A549, NCI-H460 xenografted BALB/cA nude mice |
| 投薬量 | 50, 100, 200 mg/kg | |
| 投与方法 | p.o. | |
参考
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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] | PubMed: 35207746 |
| Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] | PubMed: 35118583 |
| Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] | PubMed: 34383271 |
| Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] | PubMed: 34731453 |
| Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z] | PubMed: 34304386 |
| TRIM21 improves apatinib treatment in gastric cancer through suppressing EZH1 stability [ Biochem Biophys Res Commun, 2021, 586:177-184] | PubMed: 34856418 |
| Oxidative Stress Induces a VEGF Autocrine Loop in the Retina: Relevance for Diabetic Retinopathy [ Cells, 2020, 9(6):E1452] | PubMed: 32545222 |
| Establishment and characterization of patient-derived cancer models of malignant peripheral nerve sheath tumors. [ Cancer Cell Int, 2020, 19;20:58] | PubMed: 32099531 |
| Establishment and characterization of NCC-MFS2-C1: a novel patient-derived cancer cell line of myxofibrosarcoma [ Hum Cell, 2020, 10.1007/s13577-020-00420-z] | PubMed: 32870449 |
| Establishment and characterization of a novel cell line, NCC-TGCT1-C1, derived from a patient with tenosynovial giant cell tumor [ Hum Cell, 2020, 10.1007/s13577-020-00425-8] | PubMed: 32886306 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。