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Purity: ≥98%
Docetaxel Trihydrate (formerly RP-56976; NSC-628503; trade name Taxotere), the trihydrated form of docetaxel which is a paclitaxel analog, is a tubulin/mitotic inhibitor with a broad spectrum of antineoplastic activities. It has been approved for use in the treatment of many types of cancers.
| ln Vitro |
Cell viability was impacted in a dose-dependent manner by both single and combined treatments with docetaxel trihydrate (RP-56976 trihydrate) and glufosfamide (GLU). In PC-3 and LNCaP cells, the IC50 of GLU is 70±4 μM and 86.8±8 μM, respectively. Conversely, the IC50 of docetaxel alone was 1.46±0.2 nM and 3.08±0.4 nM in PC-3 and LNCaP cells, respectively. When GLU and Docetaxel were co-treated, the IC50 values in PC-3 and LNCaP cells were lowered to 2.7±0.1 nM and 0.75±0.3 nM, respectively [1]. NCI-H460's half-life against cetaxel was 30 nM after 72 hours and 116 nM at 24 hours. On NCI-60 cell plates, the typical IC50 for docetaxel is 14–34 nM, according to data from the DTP data search [2].
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| ln Vivo |
The intestinal cell apoptosis induced by Docetaxel Trihydrate (RP-56976 Trihydrate) in female mice was considerably higher in the 14-hour light exposure (HALO) group compared to the 2-HALO group. After receiving docetaxel, the 2-HALO group's Bax expression increased dramatically, but not in the 14-HALO group. Conversely, docetaxel markedly elevated the expression of cleaved Caspase-3 in the 14-HALO group, but not in the 2-HALO group. Furthermore, docetaxel dramatically decreased the expression of survivin protein in the 14-HALO group but not in the 2-HALO group. When compared to the 2-HALO group treated with the same medication, the survivin expression level in the 14-HALO group treated with docetaxel was considerably lower [3]. Whereas docetaxel (DOX) was given intravenously at a dose of 7 mg/kg, piperine (PIP) was given as an intravenous bolus at 3.5 mg/kg, as well as 35 mg/kg and 3.5 mg/kg orally. Rat Sprague-Daley type. Sprague-Dawley rats were coadministered PIP at 35 mg/kg orally and docetaxel at 7 mg/kg by intravenous bolus. Their in vivo exposure is synergistically increased when PIP and docetaxel are used together [4].
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| References |
[1]. Attia RT, et al. The chemomodulatory effects of glufosfamide on docetaxel cytotoxicity in prostate cancer cells. PeerJ. 2016 Jun 29;4:e2168.
[2]. Che CL, et al. DNA microarray reveals different pathways responding to paclitaxel and docetaxel in non-small cell lung cancer cell line. Int J Clin Exp Pathol. 2013 Jul 15;6(8):1538-48. [3]. Obi-Ioka Y, et al. Involvement of Wee1 in the circadian rhythm dependent intestinal damage induced by docetaxel. J Pharmacol Exp Ther. 2013 Oct;347(1):242-8. [4]. Li C, et al. Non-linear pharmacokinetics of piperine and its herb-drug interactions with docetaxel in Sprague-Dawley rats. J Pharm Biomed Anal. 2016 Sep 5;128:286-93 |
| Molecular Formula |
C43H53NO14.3H2O
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|---|---|
| Molecular Weight |
861.93
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| CAS # |
148408-66-6
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| Related CAS # |
Docetaxel;114977-28-5;Docetaxel-d5 trihydrate
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| SMILES |
CC(O[C@@]12CO[C@@H]1C[C@@H]([C@@]3([C@@H]2[C@@H]([C@@]4(C[C@@H](C(C)=C(C4(C)C)[C@H](C3=O)O)OC([C@@H]([C@H](c5ccccc5)NC(OC(C)(C)C)=O)O)=O)O)OC(c6ccccc6)=O)C)O)=O.O.O.O
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| Synonyms |
RP56976 (NSC 628503) Trihydrate; RP56976; NSC 628503; RP-56976; NSC628503; RP 56976; NSC-628503; Docetaxel trihydrate, Trade name: Taxotere.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.90 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.90 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.90 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (2.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.08 mg/mL (2.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: ≥ 2.08 mg/mL (2.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1602 mL | 5.8009 mL | 11.6019 mL | |
| 5 mM | 0.2320 mL | 1.1602 mL | 2.3204 mL | |
| 10 mM | 0.1160 mL | 0.5801 mL | 1.1602 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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