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紫杉醇 /Paclitaxel {[allProObj[0].p_purity_real_show]}

货号:A238238 同义名: NSC 125973;NSC 125973,PTX

Paclitaxel 是一种天然抗肿瘤药物,能稳定微管蛋白 (tubulin) 的聚合,导致有丝分裂停滞和诱导细胞凋亡 (apoptosis),最终导致细胞死亡。Paclitaxel 还可诱导细胞自噬 (autophagy)。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Paclitaxel 化学结构 CAS号:33069-62-4
Paclitaxel 化学结构
CAS号:33069-62-4
Paclitaxel 3D分子结构
CAS号:33069-62-4
Paclitaxel 化学结构 CAS号:33069-62-4
Paclitaxel 3D分子结构 CAS号:33069-62-4
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Paclitaxel 纯度/质量文件 产品仅供科研

货号:A238238 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

97%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 hydrochloride ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

97%
Lys05 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Paclitaxel 生物活性

描述 Microtubules are the main constituent of mitotic apparatus in all eukaryotic cells, thus make it become an important pharmacological target for the treatment of tumor[1]. Paclitaxel can stabilize the microtubule formation through interacting with β-tubulin[2] and then promoting the polymerization and assembly of it[3]. Paclitaxel show the inhibitory effect on HMVEC proliferation with IC50 of 0.1 pM, much lower than the IC50 of 5-FU, camptothecin, cisplatin and doxorubicin[4]. Paclitaxel induces G2/M arrest of cell cycle, thus it also used in synchronization in cell cycle[5]. Paclitaxel was approved by FDA in treatment of ovarian cancer, breast cancer, non-small-cell lung cancer[6], etc..
作用机制 Paclitaxel can stabilize the microtubule formation through interacting with β-tubulin[2] and then promoting the polymerization and assembly of it[3].

Paclitaxel 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
697 Growth Inhibition Assay IC50=0.0015 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=0.00796 μM SANGER
A101D Growth Inhibition Assay IC50=0.0096 μM SANGER
A253 Growth Inhibition Assay IC50=0.01738 μM SANGER

Paclitaxel 动物研究

Dose Mice: min = 2 mg/kg[7] (i.v.), max = 75 mg/kg[8] (i.p.)
Administration i.v., i.p.
Pharmacokinetics
Animal Rats[9]
Dose 30 mg/kg
Administration p.o.
Cmax 67.0 ± 14.3 ng/ml
T1/2 4.1 ± 1.2 h
AUC0→∞ 321.2 ± 79.7 h·ng/ml
CL/F 143.3 ± 51.3 L/h/kg
Tmax 1.6 ± 0.2 h
AUC0→24h 299.8 ± 77.8 h·ng/ml
V/F 321.5 ± 102.7 L/kg

Paclitaxel 参考文献

[1]Fong KW, Leung JW, et al. MTR120/KIAA1383, a novel microtubule-associated protein, promotes microtubule stability and ensures cytokinesis. J Cell Sci. 2013 Feb 1;126(Pt 3):825-37.

[2]Snyder JP, Nettles JH, et al. The binding conformation of Taxol in beta-tubulin: a model based on electron crystallographic density. Proc Natl Acad Sci U S A. 2001 Apr 24;98(9):5312-6. Epub 2001 Apr 17.

[3]Schiff PB, Fant J, et al. Promotion of microtubule assembly in vitro by taxol. Nature. 1979 Feb 22;277(5698):665-7.

[4]Wang J, Lou P, et al. Paclitaxel at ultra low concentrations inhibits angiogenesis without affecting cellular microtubule assembly. Anticancer Drugs. 2003 Jan;14(1):13-9.

[5]Trielli MO, Andreassen PR, et al. Differential Taxol-dependent arrest of transformed and nontransformed cells in the G1 phase of the cell cycle, and specific-related mortality of transformed cells. J Cell Biol. 1996 Nov;135(3):689-700.

[6]Shi X, Sun X, et al. Regulation of paclitaxel activity by microtubule-associated proteins in cancer chemotherapy. Cancer Chemother Pharmacol. 2017 Nov;80(5):909-917.

[7]Sparreboom A, van Tellingen O, et al. Nonlinear pharmacokinetics of paclitaxel in mice results from the pharmaceutical vehicle Cremophor EL. Cancer Res. 1996 May 1;56(9):2112-5.

[8]Cividalli A, Cruciani G, et al. Greater antitumor efficacy of paclitaxel administered before epirubicin in a mouse mammary carcinoma. J Cancer Res Clin Oncol. 1998;124(5):236-44.

[9]Jin J, Cai D, et al. Comparative pharmacokinetics of paclitaxel after oral administration of Taxus yunnanensis extract and pure paclitaxel to rats. Fitoterapia. 2013 Oct;90:1-9.

Paclitaxel 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.17mL

0.23mL

0.12mL

5.86mL

1.17mL

0.59mL

11.71mL

2.34mL

1.17mL

Paclitaxel 技术信息

CAS号33069-62-4
分子式C47H51NO14
分子量 853.906
别名 NSC 125973;NSC 125973,PTX
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(122.96 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

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