Docetaxel (RP 56976)

Alias: RP56976; NSC 628503; RP-56976; NSC628503; RP 56976; NSC-628503; Docetaxel hydrate, Trade name: Taxotere.
Cat No.:V1604 Purity: ≥98%
Docetaxel (formerly known as RP56976;NSC628503; RP-56976;NSC-628503;Taxotere), a semisynthetic analog ofpaclitaxel and approved anticancer drug, is a mitotic inhibitor and tubulin inhibitor that inhibits the depolymerization of microtubules by binding to and stabilizing microtubules.
Docetaxel (RP 56976) Chemical Structure CAS No.: 114977-28-5
Product category: Microtubule Associated
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
250mg
500mg
1g
2g
Other Sizes

Other Forms of Docetaxel (RP 56976):

  • Docetaxel Trihydrate (RP 56976)
  • Docetaxel-d9 (RP-56976-d9)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

Docetaxel (formerly known as RP56976; NSC628503; RP-56976; NSC-628503; Taxotere), a semisynthetic analog of paclitaxel and approved anticancer drug, is a mitotic inhibitor and tubulin inhibitor that inhibits the depolymerization of microtubules by binding to and stabilizing microtubules. Docetaxel has shown potent and a broad spectrum of antineoplastic activities and has been extensively used in the treatment of various cancers. It is a semi-synthetic, second-generation taxane derived from a compound found in the European yew tree Taxus baccata. Docetaxel displays potent and broad antineoplastic properties; it binds to and stabilizes tubulin, thereby inhibiting microtubule disassembly which results in cell- cycle arrest at the G2/M phase and cell death.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Docetaxel (RP-56976) and glufosfamide (GLU) treatments, both single and combination, had dose-dependent effects on cell survival. In PC-3 and LNCaP cells, the IC50 of GLU is 70±4 μM and 86.8±8 μM, respectively. Simultaneously, docetaxel alone had an IC50 of 3.08±0.4 nM in PC-3 and 1.46±0.2 nM in LNCaP cells. GLU and Docetaxel therapy together can enhance cytotoxicity; as a result, PC-3 and LNCaP cell IC50 values were lowered to 2.7 and 2.7, respectively. 0.75±0.3 nM and ±0.1 nM[1]. For NCI-H460, the docetaxel IC50 is 30 nM at 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].
ln Vivo
The intestinal cell apoptosis caused by docetaxel (RP-56976) in female mice was considerably higher in the 14-hour after light exposure (HALO) group compared to the 2-HALO group. Docetaxel markedly elevated Bax expression in the 2-HALO group, 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. At 14 HALO, but not at 2 HALO, docetaxel treatment resulted in a substantial increase in the expression of Wee1 and phosphorylated CKD1. Furthermore, docetaxel markedly decreased the expression of survivin in the 14-HALO group but not in the 2-HALO group. When compared to the 2-HALO group treated with the medication, the survivin expression level in the 14-HALO group treated with docetaxel was significantly lower [3]. The Sprague-Daley mouse received intravenous docetaxel (DOX) at a dose of 7 mg/kg, while piperine (PIP) was given orally at 35 mg/kg and 3.5 mg/kg and as an intravenous bolus of 3.5 mg/kg. 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].
Animal Protocol
Dissolved in 50 mg/mL stock solution in ethanol by adding an equal volume of polysorbate 80 and diluting with 5% dextrose in water to the final volume; 33 mg/kg; i.v. injection
Human colon carcinomas xenografts CX-1
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 NSC 125973 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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C43H53NO14
Molecular Weight
807.88
CAS #
114977-28-5
SMILES
O=C(O[C@@H](C1[C@@]2(C)[C@@H](O)C[C@@]3([H])OC[C@]31OC(C)=O)[C@]4(O)C[C@H](OC([C@H](O)[C@@H](NC(OC(C)(C)C)=O)C5=CC=CC=C5)=O)C(C)=C(C4(C)C)[C@@H](O)C2=O)C6=CC=CC=C6
Chemical Name
(2aR,4S,4aS,6R,9S,11S,12S,12bS)-12b-acetoxy-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate.
Synonyms
RP56976; NSC 628503; RP-56976; NSC628503; RP 56976; NSC-628503; Docetaxel hydrate, Trade name: Taxotere.
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)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (123.8 mM)
Water:<1 mg/mL
Ethanol:53 mg/mL (65.6 mM)
Solubility (In Vivo)
5%DMSO+30%PEG 300+5%Tween 80+ddH2O:2 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.2378 mL 6.1890 mL 12.3781 mL
5 mM 0.2476 mL 1.2378 mL 2.4756 mL
10 mM 0.1238 mL 0.6189 mL 1.2378 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.

Calculator

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g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.

Biological Data
  • Docetaxel

  • Docetaxel

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