Capmatinib
作者：齊岳
發(fā)布時(shí)間：2023-08-30
09:02:49
點(diǎn)擊數(shù)：
產(chǎn)品名稱(chēng)：Capmatinib
產(chǎn)品描述：
| 產(chǎn)品描述 | Capmatinib is an orally bioavailable inhibitor of the proto-oncogene c-Met (HGFR)with potential antineoplastic activity. |
| 靶點(diǎn)活性 | c-Met:0.13 nM |
| 體外活性 | 在c-MET依賴(lài)的小鼠腫瘤模型中,口服INCB28060（0.03 mg/kg）能夠有效抑制腫瘤生長(zhǎng). |
| 體內(nèi)活性 | 在腫瘤細(xì)胞中,INCB28060通過(guò)下調(diào)c-MET磷酸化以及c-MET介導(dǎo)的信號(hào)轉(zhuǎn)導(dǎo),抑制細(xì)胞增殖和存活。 |
| 激酶實(shí)驗(yàn) | c-Met Kinase Assay: The assay buffer contains 50 mM Tris-HCl, 10 mM MgCl2, 100 mM NaCl, 0.1 mg/ml BSA, 5 mM DTT, pH 7.8. For HTS 0.8 μL of 5 mM of INCB28060 dissolved in DMSO are dotted on 384-well plates. DMSO titration suggests that the maximum tolerated concentration of the solvent is 4%. To measure IC50s the INCB28060 plate is prepared by 3-fold and 11-point serial dilutions. 0.8 μL of INCB28060 in DMSO is transferred from INCB28060 plate to the assay plate. The final concentration of DMSO is 2%. Solutions of 8 nM unphosphorylated c-Met or 0.5 nM phosphorylated c-Met are prepared in assay buffer. A 1 mM stock solution of peptide substrate Biotin-EQEDEPEGDYFEWLE-amide dissolved in DMSO is diluted to 1 μM in assay buffer containing 400 μM ATP (unphosphorylated c-Met) or 160 uM ATP (phosphorylated c-Met). A 20 μL volume of enzyme solution (or assay buffer for the enzyme blank) is added to the appropriate wells in each plate and then 20 μL/well of substrate solution to initiate the reaction. The plate is protected from light and incubated at 25 °C for 90 minutes. The reaction is stopped by adding 20 μL of a solution containing 45 mM EDTA, 50 mM Tris-HCl, 50 mM NaCl, 0.4 mg/ml BSA, 200 nM SA-APC and 3 nM EUPy20. The plate is incubated for 15-30 minutes at room temperature and HTRF (homogenous time resolved fluorescence) is measured on a Perkin Elmer Fusion α-FP instrument. The HTRF program settings used are as follows: Primary excitation filter 330/30, Primary window: 200 uSec, Primary delay: 50 uSec, Number of flashes: 15, Well read time: 2000 |
| 細(xì)胞實(shí)驗(yàn) | H441 cells are seeded in RPMI-1640 medium containing 10% FBS and grown to complete confluence. Gaps are introduced by scraping cells with a P200 pipette tip. Cells are then stimulated with 50 ng/mL recombinant human HGF to induce migration across the gap in the presence of various concentrations of INCB28060. After an overnight incubation, representative photographs are taken and a semiqualitative assessment of inhibition of cell migration is conducted.(Only for Reference) |
| 別名 | INCB28060, NVP-INC280, 卡馬替尼, INC-280 |
| 分子量 | 412.42 |
| 分子式 | C23H17FN6O |
| CAS No. | 1029712-80-8 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 4.12 mg/mL (10 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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