| 名稱 | Paclitaxel |
| 描述 | Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy. |
| 細胞實驗 | 1×10^4 cells are plated in 100 μL of the growth medium in the presence or absence of increasing concentrations (0.1-1 μM) of taxol in 96-well plates and cultured at 37°C in 5% CO2 for 12-48 h. The cells are then incubated with 25 μL of MTT (5 mg/mL) at 37°C for 4 h. After dissolving the crystals with 0.04 N HCl in isopropanol, the plates are read in a microplate reader at 570 nm [1]. |
| 激酶實驗 | To determine which caspases are involved in apoptosis induced by taxol, caspase-3 inhibitor (DEVD-CHO), caspase-6 inhibitor (Z-VEID-FMK), caspase-8 inhibitor (Z-IETD-FMK or IETD-CHO), caspase-9 inhibitors (Z-LEHD-FMK or LEHD-CHO), and caspase-10 inhibitor (Z-AEVD-FMK) are used. These caspase inhibitors are dissolved in dimethyl sulfoxide (Me2SO); the final concentration of Me2SO is 0.1%. Cells (5×105) are preincubated in the presence or absence of 100 μM?each of these inhibitors for 3 h at 37°C then treated with or without 0.1, 0.5, and 1 μM?Paclitaxel for 48 h and processed for annexin V binding assay [1]. |
| 動物實驗 | Adult (250-320 g) male Sprague-Dawley rats are used for all experiments. One week following the DiI injection, rats are anesthetized with isofluorane and injected into the tail vein with 2 mg/kg paclitaxel or its vehicle (1:1:23, cremophor EL:ethanol:0.9% saline). The tail vein injection is repeated three more times every other day for a total of four injections [4]. |
| 體外活性 | 方法：人 T 細胞淋巴細胞白血病細胞 CCRF-HSB-2 用 Paclitaxel (0.01-1 μM) 處理 48 h，使用 MTT 方法檢測細胞生長抑制情況。
結(jié)果：Paclitaxel 劑量依賴性地抑制 CCRF-HSB-2 細胞生長，IC50 為 0.25 μM。[1]
方法：人胃癌細胞 AGS 用 Paclitaxel (10-160 nM) 處理 24-48 h，使用 Western Blot 方法檢測靶點蛋白表達水平。
結(jié)果：Paclitaxel 誘導凋亡相關(guān)蛋白 cleaved caspase-3 和 cleaved PARP 表達上調(diào)。[2]
方法：犬乳腺腫瘤細胞 CHMm 用 Paclitaxel (0.01-1 μM) 處理 24 h，使用 Flow Cytometry 方法檢測細胞凋亡情況。
結(jié)果：Paclitaxel 劑量依賴性誘導 CHMm 細胞凋亡。[3] |
| 體內(nèi)活性 | 方法：為研究低劑量 Paclitaxel 對腫瘤侵襲的影響，將 Paclitaxel (2.6 mg/kg) 腹腔注射給藥給攜帶膽管癌腫瘤 EGI-1 的 SCID 小鼠，每天一次，持續(xù)兩周。
結(jié)果：低劑量 Paclitaxel 治療減少了 EGI-1 細胞的肺擴散，而不顯著影響其局部腫瘤生長。[4]
方法：開發(fā) Paclitaxel 醇誘導的負面情感癥狀的臨床前模型，將 Paclitaxel (2-8 mg/kg in 1 volume ethanol+1 volume Emulphor-620 +18 volumes distilled water) 腹腔注射給 C57BL/6J 小鼠，每兩天一次，共注射四次。
結(jié)果：8 mg/kg Paclitaxel 處理導致機械性和冷性異常性疼痛的發(fā)展和維持。Paclitaxel 也誘導了焦慮樣行為和抑郁樣行為。Paclitaxel 在小鼠情感狀態(tài)建模試驗中產(chǎn)生了行為改變，而傷害性反應的增加持續(xù)時間更長。[5] |
| 存儲條件 | keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 21.4 mg/mL (25 mM)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 8.54 mg/mL (10 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO : 41.66 mg/mL (48.79 mM), Heating is recommended.
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| 關(guān)鍵字 | ADC Cytotoxin | Microtubule/Tubulin | Apoptosis | Inhibitor | NSC-125973 | ADC Payload | Paclitaxel | Autophagy | NSC125973 | inhibit |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Valproic Acid | L-Glutamic acid | Gefitinib | Hydroxychloroquine | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | L-Ascorbic acid | Paeonol | Sodium 4-phenylbutyrate |
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