Docetaxel

Modify Date: 2024-01-02 14:57:13

Docetaxel Structure
Docetaxel structure
 Common Name Docetaxel
CAS Number 114977-28-5 Molecular Weight 807.879
Density 1.4±0.1 g/cm3 Boiling Point 900.5±65.0 °C at 760 mmHg
Molecular Formula C43H53NO14 Melting Point 186-192 °C (dec.)
MSDS USA Flash Point 498.4±34.3 °C

 Use of Docetaxel


Docetaxel is an antineoplastic drug by inhibiting microtubule depolymerization, and attenuating of the effects of bcl-2 and bcl-xL gene expression.

 Names

Name docetaxel anhydrous
Synonym More Synonyms

 Docetaxel Biological Activity

Description Docetaxel is an antineoplastic drug by inhibiting microtubule depolymerization, and attenuating of the effects of bcl-2 and bcl-xL gene expression.
Related Catalog
Target

Microtubule[1]
In Vitro Docetaxel (DOC) 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].
In Vivo In female mice, the Docetaxel-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].
Cell Assay Single-drug concentration-response curves are assessed. Seeding is done at a density of 2,000 cells/well for PC-3 and LNCaP, in 96-well plates. Cells are treated with each single drug and their combination for 72 h at different drug concentrations. Docetaxel is used at concentrations of 0.1-1,000 nM. GLU is used at concentrations of 0.1-300 µm. Cytotoxicity is assessed at the end of drug exposure using SRB assay. Following 72 h exposure the cells are fixed with 10% trichloroacetic acid (150 µL) for 1 h at 4°C. Then, cells are stained for 10 min at room temperature with 0.4% SRB dissolved in 1% acetic acid. The plates are then air dried for 24 h and the dye is made soluble with 150 µL Tris (10 mM, PH 7.4) for 5 min on a shaker at 1,600 rpm. Absorbance is then measured at 545 nM using microplate reader. Results are expressed as the relative percentage of absorbance compared to control[1].
Animal Admin Mice[3] Five-week-old male Balb/c mice are used. Docetaxel (0, 10, 20, 30, 40, 60, and 80 mg/kg per week) is given once a week for 3 weeks for mice. Because more than 30 mg/kg per week of Docetaxel causes body weight loss in mice, 20 mg/kg per week of Docetaxel is judged to be the maximum nontoxic dose. Docetaxel (20 mg/kg per week) is given to mice once a week for 3 weeks at one of the following different points (2, 10, 14, or 22 HALO). Seventy-two hours after the final dosing of the agent, the intestinal mucosa of the small intestine (proximal 8 cm) is removed, fixed in 20 N Mildform solution (containing 8% formaldehyde in a buffered solution), and embedded in paraffin blocks, and sections of 5 μm are put on glass slides. Apoptosis is detected using the terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) method, using the Apop Tag Peroxidase In Situ Apoptosis Detection Kit. Rats[4] Male Sprague-Dawley rats with body weight between 230-250 g and age between 6-7 weeks are used. About 25 SD rats are divided into five groups receiving Docetaxel (7 mg/kg, i.v.), PIP (35 mg/kg, p.o.) and their combined administration (DOX+PIP) as well as PIP (3.5 mg/kg, p.o.) and PIP (3.5 mg/kg, i.v.). A day before the drug administrations, the rats are anesthetized with an intramuscular injection of a cocktail containing 60 mg/kg ketamine and 6 mg/kg xylazine (injection volume, 0.2 mL). Right jugular vein is cannulated with a polyethylene tubing (0.5 mm ID, 1 mm) for blood collection.
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.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 900.5±65.0 °C at 760 mmHg
Melting Point 186-192 °C (dec.)
Molecular Formula C43H53NO14
Molecular Weight 807.879
Flash Point 498.4±34.3 °C
Exact Mass 807.346619
PSA 224.45000
LogP 6.55
Vapour Pressure 0.0±0.3 mmHg at 25°C
Index of Refraction 1.618
Storage condition 2~8°C

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes Xi:Irritant
Risk Phrases R36/37/38
Safety Phrases 26-36/37
RIDADR 1544
RTECS DA4172750
Packaging Group III
Hazard Class 6.1(b)
HS Code 2932999099

 Customs

HS Code 2932999099
Summary 2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles224

More Articles
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Androgen receptor (AR) networks are predominantly involved in prostate cancer (PCa) progression; consequently, factors of AR regulation represent promising targets for PCa therapy. The ErbB3-binding p...
Immediate and transient phosphorylation of the heat shock protein 27 initiates chemoresistance in prostate cancer cells.

Oncol. Rep. 32(6) , 2380-6, (2014)

Drug resistance minimizes the effects of prostate cancer (PC) chemotherapy with docetaxel and is generally considered to be associated with the expression of heat shock protein (HSP) 27 including vari...
Inhibition of PI3Kβ signaling with AZD8186 inhibits growth of PTEN-deficient breast and prostate tumors alone and in combination with docetaxel.

Mol. Cancer Ther. 14(1) , 48-58, (2015)

Loss of PTEN protein results in upregulation of the PI3K/AKT pathway, which appears dependent on the PI3Kβ isoform. Inhibitors of PI3Kβ have potential to reduce growth of tumors in which loss of PTEN ...

 Synonyms

(5β,7β,10β,13α)-4-Acetoxy-13-({(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1,7,10-trihydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate
Benzenepropanoic acid, β-[[(1,1-dimethylethoxy)carbonyl]amino]-α-hydroxy-, (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-yl ester, (αR,βS)-
Benzenepropanoic acid, β-[[(1,1-dimethylethoxy)carbonyl]amino]-α-hydroxy-, (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,6, 11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-yl ester, (αR,βS)-
D-2-amino-5-phosphonovaleric acid
APV
AP-5
DL-APV
(2α,5β,7β,10β,13α)-4-Acetoxy-13-({(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1,7,10-trihydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate
MFCD00800737
DOCETAXEL TRIHYDRATE
Docetaxol
5-PHOSPHONO-DL-NORVALINE
Taxotere
(2α,5β,7β,10β,13α)-4-Acetoxy-1,7,10-trihydroxy-13-{[(2R,3S)-2-hydroxy-3-({[(2-methyl-2-propanyl)oxy]carbonyl}amino)-3-phenylpropanoyl]oxy}-9-oxo-5,20-epoxytax-11-en-2-yl benzoate
DL-2-amino-5-phosphonovaleric acid
DOCETAXEL(TAXOTERE)
N-Debenzoyl-N-tert-butoxycarbonyl-10-deacetyltaxol
Docetaxel
N-DEBENZOYL-N-TERT-BUTOXYCARBONYL-10-DEACETYL
DOCETAXEL(TAXOTERE) UK 427857
N-debenzoyl-N-Boc-10-deacetyl taxol
TAXOTERE, DOCETAXEL
(2α,5β,7β,10β,13α)-4-(acetyloxy)-13-({(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1,7,10-trihydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate
2-amino-5-phosphopentanoicacid
N-debenzoyl-N-tert-butoxycarbonyl-10-deacetyl taxol
2-amino-5-phosphonovaleric acid
acide amino-6 carboxy-6 hexylphosphonique
2-amino-5-phosphovaleric acid
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Related Compounds: More...
Docetaxel
125354-16-7
Docetaxel
114915-14-9
Docetaxel-d9
940867-25-4
[3H]-Docetaxel
133577-33-0
[3H]-Docetaxel
114915-20-7
7-Epidocetaxel
153381-68-1
2'-TBS-docetaxel
342613-14-3
2’-TES-docetaxel
162871-12-7
2'-THP-docetaxel
1372883-34-5
Chemsrc provides Docetaxel(CAS#:114977-28-5) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of Docetaxel are included as well.>> amp version: Docetaxel

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