Docetaxel  (Synonyms: RP-56976)

Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC₅₀ of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity^[1][3].

Microtubule^[1]

Docetaxel (RP-56976) and Glufosfamide (GLU) single and combined treatments affect the cells viability in a dose-dependent manner. The IC₅₀ of GLU are 70±4 μM and 86.8±8 μM in PC-3 and LNCaP cells; respectively. While, the IC₅₀ of Docetaxel alone is found to be 3.08±0.4 nM and 1.46±0.2 nM in PC-3 and LNCaP cells; respectively.
The co-treatment of GLU with Docetaxel is found to synergize the cytotoxicity and the IC₅₀ values are decreased to be 2.7±0.1 nM and 0.75±0.3 nM in PC-3 and LNCaP cells; respectively^[1].
IC₅₀ of NCI-H460 to Docetaxel at 24 h is 116 nM and at 72 h is 30 nM. According to data reported in DTP Data Search, the mean IC₅₀ of NCI-60 cell panel to Docetaxel is 14-34 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In female mice, the Docetaxel (RP-56976)-induced intestinal apoptosis in the 14-hours after light on (HALO) group is significantly greater than that in the 2-HALO group. Bax expression is significantly elevated by Docetaxel in the 2-HALO group, but not in the 14-HALO group. On the other hand, cleaved Caspase-3 expression is significantly elevated by Docetaxel in the 14-HALO group, but not in the 2-HALO group. The expressions of Wee1 and phosphorylated CKD1 are significantly elevated after dosing of Docetaxel at 14 HALO, but not at 2 HALO. In addition, Docetaxel significantly reduces survivin expression in the 14-HALO group but not in the 2-HALO group. The survivin expression level in the Docetaxel-treated 14-HALO group is significantly smaller than that in the drug-treated 2-HALO group^[3].
Piperine (PIP) is administrated via intravenous bolus at 3.5 mg/kg and via oral administration at 35 mg/kg and 3.5 mg/kg, while Docetaxel (DOX) is intravenously administrated at 7 mg/kg to Sprague-Daley rats. The co-administrations of PIP at 35 mg/kg via oral administration and Docetaxel at 7 mg/kg via intravenous bolus administration in Sprague-Dawley rats. The combination use of PIP and Docetaxel results in a synergic increase of both their in vivo exposure^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

807.88

C₄₃H₅₃NO₁₄

114977-28-5

Solid

White to off-white

O=C(OC(C)(C)C)N[C@@H](C1=CC=CC=C1)[C@H](C(O[C@@H]2C(C)=C([C@@H](O)C([C@@]3(C)[C@]([C@@](CO4)(OC(C)=O)[C@@]4([H])C[C@@H]3O)([H])[C@@H]5OC(C6=CC=CC=C6)=O)=O)C(C)(C)[C@@]5(O)C2)=O)O

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

• [1]. Attia RT, et al. The chemomodulatory effects of glufosfamide on docetaxel cytotoxicity in prostate cancer cells. PeerJ. 2016 Jun 29;4:e2168.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]