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

货号:A238238 同义名: 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)。Paclitaxel通过微管聚合抑制体外神经突的启动和生长。

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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/紫杉醇 化学结构 CAS号:33069-62-4
Paclitaxel/紫杉醇 化学结构
CAS号:33069-62-4
Paclitaxel/紫杉醇 3D分子结构
CAS号:33069-62-4
Paclitaxel/紫杉醇 化学结构 CAS号:33069-62-4
Paclitaxel/紫杉醇 3D分子结构 CAS号:33069-62-4
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Paclitaxel/紫杉醇 纯度/质量文件 产品仅供科研

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产品名称 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

95%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 HCl ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

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

Autophagy, IC50: 40 nM

99%
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/紫杉醇 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/紫杉醇 细胞实验

Cell Line
Concentration Treated Time Description References
HCT15 cells 50 µg/ml 24 hours To compare the apoptosis-inducing effects of UTD1 and paclitaxel in ABCB1 high-expression cells, UTD1 showed stronger apoptosis-inducing ability Cell Death Dis. 2021 Apr 1;12(4):338.
KPC tumor cells 10μM 36 hours To evaluate the effect of paclitaxel on Cytidine deaminase protein levels, results showed paclitaxel reduced Cda protein levels through ROS-mediated degradation Cancer Discov. 2012 Mar;2(3):260-269.
BxPC3 cells 3-50 μg/ml 48 h To evaluate the drug delivery efficacy of PEI-MSNP in BxPC3 cells, results showed that PEI-MSNP effectively delivered Paclitaxel, leading to increased cytotoxicity. ACS Nano. 2009 Oct 27;3(10):3273-86.
PANC-1 cells 3-50 μg/ml 48 h To evaluate the drug delivery efficacy of PEI-MSNP in PANC-1 cells, results showed that PEI-MSNP effectively delivered Paclitaxel, leading to increased cytotoxicity. ACS Nano. 2009 Oct 27;3(10):3273-86.
H460 cells 5 μM 48 h To evaluate the cytotoxicity of PTX/TPGS nanocrystals on H460 cells, results showed significant inhibition of H460 cell proliferation. Mol Pharm. 2010 Jun 7;7(3):863-9.
KB cells 5 μM 48 h To evaluate the cytotoxicity of PTX/TPGS nanocrystals on KB cells, results showed significant inhibition of KB cell proliferation. Mol Pharm. 2010 Jun 7;7(3):863-9.
NCI/ADR-RES cells 5 μM 48 h To evaluate the cytotoxicity of PTX/TPGS nanocrystals on drug-resistant cancer cells, results showed significant inhibition of NCI/ADR-RES cell proliferation. Mol Pharm. 2010 Jun 7;7(3):863-9.
4T1 cells with M2 macrophages derived from RAW264.7 cells 2.5 μM + 2.5 μM 14 days The combination of IPI-549 and paclitaxel (PTX) completely inhibited the growth of 3D multicellular tumor spheroids (MTCs), while IPI-549 or PTX alone showed limited inhibition. Sci Transl Med. 2022 May 4;14(643):eabl3649.
Bone marrow-derived macrophages (BMDMs) 5 μM The combination of IPI-549 with paclitaxel (PTX) enhanced the repolarization of M2 macrophages to M1 macrophages, as indicated by an increase in M1 markers (TNF-α and IL-12) and a decrease in M2 markers (IL-10 and TGF-β). Sci Transl Med. 2022 May 4;14(643):eabl3649.
A549 cells 10 –80 ng/mL 48 h To investigate the effect of Paclitaxel on CTSL expression in A549 cells, results showed that Paclitaxel treatment induced CTSL expression. Acta Pharmacol Sin. 2016 Dec;37(12):1606-1622.

Paclitaxel/紫杉醇 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Chemotherapy-induced bile acid metabolism disorder model Intraperitoneal injection 30 mg/kg Every other day, total six doses To investigate the effect of chemotherapy on bile acid metabolism, results showed chemotherapy reduced the level of secondary bile acid HDCA Gut Microbes. 2024 Jan-Dec;16(1):2410475
Nude mice NCI/ADR-RES xenograft model Intravenous injection 10 mg/kg Administered on days 0, 3, 6, 9, 12 To evaluate the antitumor efficacy of PTX/TPGS nanocrystals in the NCI/ADR-RES xenograft model, results showed significant tumor growth inhibition. Mol Pharm. 2010 Jun 7;7(3):863-9.
Mice MDA-MB-231 xenograft Oral ceritinib + Intraperitoneal paclitaxel 10 mg/kg Ceritinib once daily for 2 weeks; paclitaxel twice weekly for 2 weeks To evaluate the inhibitory effect of ceritinib and paclitaxel combination therapy on ARlow TNBC tumor growth. Results showed that the combination treatment significantly inhibited tumor growth and lung metastasis. Mol Cancer. 2022 Jun 29;21(1):138.
Mice MMTV-PyMT transgenic mice with spontaneous breast cancer and lung metastasis Intravenous injection 10 mg/kg Once every 3 days for five doses The combination of Nano-PI with α-PD1 achieved long-term tumor remission, eliminated lung metastasis, and significantly improved survival in MMTV-PyMT transgenic mice. Sci Transl Med. 2022 May 4;14(643):eabl3649.
Mice Cognitive impairment model Intraperitoneal injection 20 mg/kg Every other day for 4 doses To investigate the mechanism of paclitaxel-induced cognitive impairment and evaluate the therapeutic effects of lithium and PKC inhibitors. Results showed that paclitaxel injections impaired short-term spatial memory in mice, altered neuronal morphology in the hippocampus and prefrontal cortex, and upregulated PKCα expression. Pretreatment with lithium and PKC inhibitors rescued these deficits. Mol Neurodegener. 2021 Jun 26;16(1):41
BALB/c nude mice A549 cell xenograft model Intraperitoneal injection 10 mg/kg, 15 mg/kg Every 3 days for 2 weeks To investigate the effect of Paclitaxel on A549 cells overexpressing CTSL in a xenograft model, results showed that overexpression of CTSL reduced sensitivity to Paclitaxel. Acta Pharmacol Sin. 2016 Dec;37(12):1606-1622.

Paclitaxel/紫杉醇 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/紫杉醇 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/紫杉醇 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/紫杉醇 技术信息

CAS号33069-62-4
分子式C47H51NO14
分子量 853.91
SMILES Code O=C1[C@H](OC(C)=O)C(C2(C)C)=C(C)[C@@H](OC([C@H](O)[C@@H](NC(C3=CC=CC=C3)=O)C4=CC=CC=C4)=O)C[C@@]2(O)[C@@H](OC(C5=CC=CC=C5)=O)[C@@]6([H])[C@@]1(C)[C@@H](O)C[C@@]7([H])OC[C@]76OC(C)=O
MDL No. MFCD00869953
别名 NSC 125973; PTX
运输蓝冰
InChI Key RCINICONZNJXQF-MZXODVADSA-N
Pubchem ID 36314
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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