ZM 306416

製品コードS2897 バッチS289703

印刷

化学情報

Chemical Structure Synonyms CB 676475 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H13ClFN3O2
分子量 333.74 CAS No. 690206-97-4
Solubility (25°C)* 体外 DMSO 67 mg/mL (200.75 mM)
Water Insoluble
Ethanol Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 ZM 306416 (CB 676475) is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.
in vitro ZM-306416 induces selective antiproliferative effect toward the EGFR-addicted NSCLC cell lines H3255 and HCC4011 with IC50 of 0.09 µM and 0.072 µM, respectively. ZM-306416 inhibits granule formation with IC50 of 0.67 μM. [1] ZM-306416 significantly inhibits the ERRα assay with IC50 of 7.3 μM in the GeneBLAzer T-Rex RORγ-UAS-bla HEK293T cell line. [2] ZM306416 (300 nM) completely inhibits PAA secretion and stimulates [125]I uptake in human thyroid follicular cells. ZM306416 (300 nM) abolishes pVEGFR2 (Y1214) expression in human thyroid follicular cells. ZM306416 (< 10 μM) has marked inhibitory effects on the steady state phosphorylation of p42/44 MAPK but does not affect the expression of the unphosphorylated form. ZM306416 (3 μM) significantly increases cell death in human thyroid follicular cells. ZM306416 (3 μM) significantly increases cell death in human thyroid follicular cells. ZM306416 weakly inhibits the secretion of VEGF and increases the production of PlGF. [3] ZM306416 (1 μM) enhances follicle formation and decreased nuclear distribution in human thyroid follicular cells. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
The potency of ZM-306416 is measured in dose-response studies in a 384-well format using 12 doubling dilutions in duplicate with a 10 µM and 1 µM ZM-306416 concentration as the upper limit. All reagents transfers are performed using the PP-384-M Personal Pipettor. ZM-306416 or controls are added to the wells at a volume of 1 µL to white 384-well microplates. Controls consisted of 1% DMSO (v/v) (high control) and 30 µM staurosporine in 1% DMSO (v/v) (low controls). The assay buffer is 25 mM HEPES/NaOH (pH 7.5) and contained 10 mM MgCl2, 2 mM TCEP, 20 mM β-glycerol phosphate, and 100 µM Na3VO4; for each kinase on the panel, 4 µL kinase dilution in assay buffer is added to the wells to reach a final concentration of 50 nM enzyme. After enzyme addition, kinase and ZM-306416 are preincubated for 10 min at room temperature. Then, 5 µL of a mix containing ATP and Poly(Glu, Tyr) substrates in solution in assay buffer is added to the wells to reach a final concentration of 200 µM. After a 45 min reaction at room temperature, 10 µM ADP-Glo Reagent is added to each well. After a 40-min incubation, 20 µM Kinase Detection Reagent is added followed by a 60-min incubation. The luminescence signal output is measured on the LEADseeker multimodality imaging system.

カスタマーフィードバック

, , Sci Rep, 2015, 5:7890.

, , Cell Signal, 2016, 28(6):652-62.

Data from [Data independently produced by , , PLoS One, 2016, 11(9):e0161332]

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Establishment of an oral squamous cell carcinoma cell line expressing vascular endothelial growth factor a and its two receptors [ J Dent Sci, 2022, 17(4):1471-1479] PubMed: 36299342
Vascular endothelial growth factor B exerts lipid-lowering effect by activating AMPK via VEGFR1 [ Life Sci, 2021, 276:119401] PubMed: 33785341
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The in vitro effect of VEGF receptor inhibition on primary alveolar osteoblast nodule formation. [ Aust Dent J, 2020, 10.1111/adj.12752] PubMed: 32072641
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Activated T cells induce proliferation of oligodendrocyte progenitor cells via release of vascular endothelial cell growth factor-A. [ Glia, 2018, 66(11):2503-2513] PubMed: 30500113
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Cooperative Effects of Vascular Angiogenesis and Lymphangiogenesis [ Regen Eng Transl Med, 2018, 4(3):120-132] PubMed: 30417074

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。