DHA-paclitaxel is an inert prodrug composed of the natural fatty acid DHA covalently linked to the C2′-position of paclitaxel. The paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Compared to Paclitaxel, DHA-Paclitaxel targets tumor cells more specifically because tumor cells absorb large amounts of natural fatty acids for use as biochemical precursors and energy sources.
分子量
1164.38
Formula
C69H81NO15
CAS 号
199796-52-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Sparreboom A, Wolff AC, Verweij J, et al. Disposition of docosahexaenoic acid-paclitaxel, a novel taxane, in blood: in vitro and clinical pharmacokinetic studies. Clin Cancer Res. 2003;9(1):151-159.
[2]. Bradley MO, Webb NL, Anthony FH, et al. Tumor targeting by covalent conjugation of a natural fatty acid to paclitaxel. Clin Cancer Res.
DHA-paclitaxel is an inert prodrug composed of the natural fatty acid DHA covalently linked to the C2′-position of paclitaxel. The paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Compared to Paclitaxel, DHA-Paclitaxel targets tumor cells more specifically because tumor cells absorb large amounts of natural fatty acids for use as biochemical precursors and energy sources.
分子量
1164.38
Formula
C69H81NO15
CAS 号
199796-52-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Sparreboom A, Wolff AC, Verweij J, et al. Disposition of docosahexaenoic acid-paclitaxel, a novel taxane, in blood: in vitro and clinical pharmacokinetic studies. Clin Cancer Res. 2003;9(1):151-159.
[2]. Bradley MO, Webb NL, Anthony FH, et al. Tumor targeting by covalent conjugation of a natural fatty acid to paclitaxel. Clin Cancer Res.
DHA-paclitaxel is an inert prodrug composed of the natural fatty acid DHA covalently linked to the C2′-position of paclitaxel. The paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Compared to Paclitaxel, DHA-Paclitaxel targets tumor cells more specifically because tumor cells absorb large amounts of natural fatty acids for use as biochemical precursors and energy sources.
分子量
1164.38
Formula
C69H81NO15
CAS 号
199796-52-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Sparreboom A, Wolff AC, Verweij J, et al. Disposition of docosahexaenoic acid-paclitaxel, a novel taxane, in blood: in vitro and clinical pharmacokinetic studies. Clin Cancer Res. 2003;9(1):151-159.
[2]. Bradley MO, Webb NL, Anthony FH, et al. Tumor targeting by covalent conjugation of a natural fatty acid to paclitaxel. Clin Cancer Res.
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生物活性
Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy[1][2].
IC50 & Target[1]
Traditional Cytotoxic Agents
体外研究 (In Vitro)
Paclitaxel (20 nM; 48 hours) induces programmed cell death and exists a block at the G2/M phase of the cell cycle[1]. Paclitaxel (20 nM; 48 hours) induces a consistent increase in the level of p53[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis[1]
Cell Line:
MCF-7, MDA-MB-231 cells
Concentration:
20 nM
Incubation Time:
48 hours
Result:
Induced programmed cell death.
Cell Cycle Analysis[1]
Cell Line:
MCF-7, MDA-MB-231 cells
Concentration:
20 nM
Incubation Time:
48 hours
Result:
>60% of MCF-7 cells and 50% of MDA-MB-231 cells were in the G2/M phase following 24 h treament.
Western Blot Analysis[1]
Cell Line:
MCF-7 cells (harboring wild-type p53)
Concentration:
20 nM
Incubation Time:
48 hours
Result:
Induced a consistent increase in the level of p53.
体内研究 (In Vivo)
Paclitaxel (1-20 mg/kg; i.p.; 1 time/2 days for five cycles) obviously induces liver metastases at the low-Paclitaxel group with little influence on primary tumor growth[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
MDA-231 xenograft-bearing mice[3]
Dosage:
1, 20 mg/kg
Administration:
Intraperitoneal injection; five cycles (1 time/2 days)
Result:
Liver metastases were obviously induced in the low-PTX (1 mg/kg) group with little influence on primary tumor growth compared with high-PTX group.
Clinical Trial
分子量
853.91
Formula
C47H51NO14
CAS 号
33069-62-4
中文名称
紫杉醇
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Choi YH, et al. Paclitaxel-induced growth arrest and apoptosis is associated with the upregulation of the Cdk inhibitor, p21WAF1/CIP1, in human breast cancer cells. Oncol Rep. 2012 Dec;28(6):2163-9.
[2]. Dziadyk JM, et al. Paclitaxel-induced apoptosis may occur without a prior G2/M-phase arrest. Anticancer Res. 2004 Jan-Feb;24(1):27-36.
[3]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Aug;283(15):2836-52.
[4]. Pan Z, et al. Paclitaxel attenuates Bcl-2 resistance to apoptosis in breast cancer cells through an endoplasmic reticulum-mediated calciumrelease in a dosage dependent manner. Biochem Biophys Res Commun. 2013 Feb 13. pii: S0006-291X(13)00259-3.
[5]. Cadamuro M, et al. Low dose paclitaxel reduces S100A4 nuclear import to inhibit invasion and hematogenous metastasis of cholangiocarcinoma. Cancer Res. 2016 Jun 21.
[6]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Jun 16.
[7]. Yilmaz E, et al. Sensory neuron subpopulation-specific dysregulation of intracellular calcium in a rat model of chemotherapy-induced peripheral neuropathy. Neuroscience. 2015 Aug 6;300:210-8.
[8]. Jing C, et al. E7080 enhances the antitumor effects of paclitaxel in anaplastic thyroid cancer. Am J Cancer Res. 2017 Apr 1;7(4):903-912.
10-Deacetyl-7-xylosyl paclitaxel Chemical Structure
CAS No. : 90332-63-1
规格
价格
是否有货
数量
10 mg
¥800
In-stock
50 mg
¥2650
询价
100 mg
询价
200 mg
询价
* Please select Quantity before adding items.
10-Deacetyl-7-xylosyl paclitaxel 相关产品
•相关化合物库:
Natural Product Library Plus
Bioactive Compound Library Plus
Toxins for Antibody-Drug Conjugate Research Library
生物活性
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel (a microtubule stabilizing agent; enhances tubulin polymerization) derivative with improved pharmacological features. IC50 value: Target: Microtubule inhibitor 10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cycle arrest and apoptosis as measured by flow cytometry, DNA laddering, and transmission electron microscopy. Pro-apoptotic Bax and Bad protein expression was up-regulated and anti-apoptotic Bcl-2 and Bcl-XL expression down-regulated, which lead to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9. In turn, caspase-9 activated downstream caspases-3 and -6, but not caspase-8. Bid was also activated by caspase-3. Reversely, treatment with a caspase-10-specific inhibitor could not protect PC-3 cells from 7-xylosyl-10-deacetyl-paclitaxel-triggered apoptosis. Moreover, 7-xylosyl-10-deacetylpaclitaxel had no effect on the expression of CD95 and NF-kappaB proteins, indicating that apoptosis was induced through the mitochondrial-dependent pathway in PC-3 cells.
IC50 & Target
Traditional Cytotoxic Agents
分子量
943.98
Formula
C50H57NO17
CAS 号
90332-63-1
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Jiang S, et al. Activation of the mitochondria-driven pathway of apoptosis in human PC-3 prostate cancer cells by a novel hydrophilic paclitaxel derivative, 7-xylosyl-10-deacetylpaclitaxel. Int J Oncol. 2008 Jul;33(1):103-11.
Paclitaxel-d5 benzoyloxy is the deuterium labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy[1][2].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
858.94
Formula
C47H46D5NO14
CAS 号
1261254-56-1
中文名称
紫杉醇 d5 (苯甲酸)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Choi YH, et al. Paclitaxel-induced growth arrest and apoptosis is associated with the upregulation of the Cdk inhibitor, p21WAF1/CIP1, in human breast cancer cells. Oncol Rep. 2012 Dec;28(6):2163-9.
[3]. Dziadyk JM, et al. Paclitaxel-induced apoptosis may occur without a prior G2/M-phase arrest. Anticancer Res. 2004 Jan-Feb;24(1):27-36.
[4]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Aug;283(15):2836-52.
[5]. Pan Z, et al. Paclitaxel attenuates Bcl-2 resistance to apoptosis in breast cancer cells through an endoplasmic reticulum-mediated calciumrelease in a dosage dependent manner. Biochem Biophys Res Commun. 2013 Feb 13. pii: S0006-291X(13)00259-3.
[6]. Cadamuro M, et al. Low dose paclitaxel reduces S100A4 nuclear import to inhibit invasion and hematogenous metastasis of cholangiocarcinoma. Cancer Res. 2016 Jun 21.
[7]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Jun 16.
[8]. Yilmaz E, et al. Sensory neuron subpopulation-specific dysregulation of intracellular calcium in a rat model of chemotherapy-induced peripheral neuropathy. Neuroscience. 2015 Aug 6;300:210-8.
[9]. Jing C, et al. E7080 enhances the antitumor effects of paclitaxel in anaplastic thyroid cancer. Am J Cancer Res. 2017 Apr 1;7(4):903-912.
7-O-(Amino-PEG4)-paclitaxel is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
PEGs
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
1101.19
Formula
C58H72N2O19
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
In solvent
-80°C
6 months
-20°C
1 month
参考文献
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
Paclitaxel-d5 is a deuterium-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization[1].
分子量
858.94
Formula
C47H46D5NO14
CAS 号
1129540-33-5
中文名称
紫杉醇 d5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Choi YH, et al. Paclitaxel-induced growth arrest and apoptosis is associated with the upregulation of the Cdk inhibitor, p21WAF1/CIP1, in human breast cancer cells. Oncol Rep. 2012 Dec;28(6):2163-9.
[2]. Dziadyk JM, et al. Paclitaxel-induced apoptosis may occur without a prior G2/M-phase arrest. Anticancer Res. 2004 Jan-Feb;24(1):27-36.
Paclitaxel-d5 is a deuterium-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization[1].
分子量
858.94
Formula
C47H46D5NO14
CAS 号
1129540-33-5
中文名称
紫杉醇 d5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Choi YH, et al. Paclitaxel-induced growth arrest and apoptosis is associated with the upregulation of the Cdk inhibitor, p21WAF1/CIP1, in human breast cancer cells. Oncol Rep. 2012 Dec;28(6):2163-9.
[2]. Dziadyk JM, et al. Paclitaxel-induced apoptosis may occur without a prior G2/M-phase arrest. Anticancer Res. 2004 Jan-Feb;24(1):27-36.
Paclitaxel-d5 is a deuterium-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization[1].
分子量
858.94
Formula
C47H46D5NO14
CAS 号
1129540-33-5
中文名称
紫杉醇 d5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Choi YH, et al. Paclitaxel-induced growth arrest and apoptosis is associated with the upregulation of the Cdk inhibitor, p21WAF1/CIP1, in human breast cancer cells. Oncol Rep. 2012 Dec;28(6):2163-9.
[2]. Dziadyk JM, et al. Paclitaxel-induced apoptosis may occur without a prior G2/M-phase arrest. Anticancer Res. 2004 Jan-Feb;24(1):27-36.