Docetaxel (RP56976)

For research use only.

Catalog No.S1148 Synonyms: NSC 628503

135 publications

Docetaxel (RP56976) Chemical Structure

CAS No. 114977-28-5

Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

Selleck's Docetaxel (RP56976) has been cited by 135 publications

Purity & Quality Control

Choose Selective Microtubule Associated Inhibitors

Biological Activity

Description Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.
Targets
Microtubules [1]
(Cell-free assay)
In vitro

Docetaxel is a cytotoxic agent, especially for proliferating cells, which is related to its ability to promote the formation of microtubule bundles and induce sustained mitotic arrest, followed by apoptosis of mitotically arrested cells or permanent mitotic block. Docetaxel suppresses microtubule dynamic instability as well as tread-milling, resulting in the failure of chromosomes to segregate to the daughter cells, which in turn triggers premature exit from mitosis rather than a block at this phase of the cell cycle. [2] Docetaxel inhibits the clonogenic survival of Human cancer cell Hs746T (stomach), AGS (stomach), HeLa (cervix), CaSki (cervix), BxPC3 (pancreas), Capan-1 (pancreas) with IC50 of 1 nM, 1 nM, 0.3 nM, 0.3 nM, 0.3 nM and 0.3 nM respectively. [4] Docetaxel inhibits endothelial cell migration that does not affects microtubule gross morphology or inhibit cell proliferation, although they does produce more subtle effects on microtubule dynamics. Docetaxel inhibits HUVEC migration with an observed IC50 of 1 pM. HUVEC chemotaxis stimulated by either of two angiogenic factors, thymidine phosphorylase or VEGF, is inhibited by Docetaxel with IC 50 of 10 pM and is ablated at 1 nM. [7] Docetaxel induces human monocytes, but not RAW 264.7 murine macrophages, Prostaglandin H Synthase-2m (PGHS-2) expression. [8]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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COLO-679 MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTBwNkKxO|Ih|ryP M4Dvc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFkzNyd-U1HOS2VTRC:jPh?=
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NY NV\re29yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXXR5NKSzVyPUCuPVM{PTJizszN MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5Nk8oRlODTlfFVlww[T5?
NCI-H1993 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zFUWlEPTB;MT6xPVI5QSEQvF2= NXHTUIpJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTJxJ{7TRW5ITVJ:L3G+
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PIM1; 

PubMed: 18426800     


Cells were treated with 100 nm docetaxel for the indicated times. PIM1 and β-ACTIN proteins were analyzed by immunoblot analysis. One of three similar blots is shown. Ratio, ratio of PIM1/β-ACTIN from pooled densitometry data from three separate experimen䲧疝Ỵ疞㧀疜膉痘瘿뾠ՂᾰƌՂĀ㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ⟸෕䐺痖暼瘿⟸෕ᾰƌ

cyclin B; 

PubMed: 18426800     


Immunoblot analysis of cyclin B1 and PIM1 expression after docetaxel 10 nm (left) or 100 nm (right) treatment at various time points.

pSTAT3 / STAT3 ; 

PubMed: 18426800     


Immunoblots of RWPE-2 cells treated with 100 nm docetaxel for the indicated time.

p-p53 / p53; 

PubMed: 22996738     


C4-2 cells were treated with 5 nM docetaxel, the whole cell lysates were collected at different time points and subjected to Western blot.

18426800 22996738
Immunofluorescence
α-tubulin; 

PubMed: 27177833     


Noscapine has no effect on gross microtubule polymerization state but noscapine pre-sensitization followed by docetaxel treatment stabilizes microtubules, hence inhibits cell proliferation. TNBC cells were treated with noscapine (4 µM) or docetaxel (0.4 µ䲧疝Ỵ疞㧀疜膉痘瘿⟸෕ᾰƌ෕Ð㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뾠Ղ䐺痖暼瘿뾠Ղᾰƌ 뾠ՂÐ㺣痖뾠Ղ€𢡄뾤Ղ€䀷痗뾤Ղ౴뾤Ղ㵶痗뾤Ղ뺖᎒泌Itemセ᎒Count﫨呂뿔Ղ猴፲뾤Ղ፲씢痗猸፲髸莤䥷堙᎒セ᎒�堞ﻮ᎒፲露𢡄堚Ҕ齃礤v�堞ﻮ᎒猢Wセ᎒䨼Ą鹿齃殺獸W戀醙

cleaved PARP / cleaved caspase-3; 

PubMed: 21087597     


Immunofluorescence images of PC-3 cells treated with the docetaxel and EM011 schedule treatment. Cells were pretreated with docetaxel for 12 h before addition of EM011 and were fixed at 48 h post docetaxel treatment compared to treatment with EM011 (10 μM䲧疝Ỵ疞㧀疜膉痘瘿⟸෕ᾰƌ෕Ð㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ�෋䐺痖暼瘿�෋ᾰƌ �෋à

Acetylated tubulin ; 

PubMed: 18426800     


Immunofluorescence of acetylated tubulin in cells treated with DMSO, 30 nM laulimalide and 30 nM docetaxel for 2.5 h. Tubulin shown in green and DAPI in blue, and the white arrow indicates microtubule bundling. Scale bar represents 10 μm.

SQSTM1 / LAMP1; 

PubMed: 29795139     


AGS cells were treated with docetaxel (10 nM) for 12 h. After immunostaining with SQSTM1 (Alexa Fluor 488, green) and LAMP1 (Alexa Fluor 594, red), cells were examined by fluorescence microscopy (scale bar 20 μm). The colocalization of SQSTM1and LAMP1 was䲧疝Ỵ疞㧀疜膉痘瘿�෋ᾰƌ෋à㺣痖帉痖Ѐ

27177833 21087597 18426800 29795139
Growth inhibition assay
Cell viability ; 

PubMed: 22996738     


Docetaxel inhibits the growth of LNCaP, C4-2, DU145, and PC3 prostate cancer cells. Cells were plated in 12-well plates and treated with different concentrations of docetaxel. The cell number was counted after 24 hr. 

22996738
In vivo Docetaxel (33 mg/kg/dose, given i.v. every 4 days for 3 injections) results in a tumor growth delay of 19.3 days in M2OL2 colon xenografts. Docetaxel also shows great antitumor activities in MX-1, SK-MEL-2, LX-1 and OVCAR-3 xenografts. Docetaxel inhibits the angiogenic response to fibroblast growth factor 2 with IC 50 of 5.4 mg/kg when injected twice weekly over a 14-day period, and angiogenesis is completely blocked in mice that receives 10 mg/kg Docetaxel. Docetaxel has selectivity for endothelial cell migration and/or microvessel formation because infiltration of inflammatory cells into the Matrigel plug is much less sensitive to inhibition by Docetaxel. [7]

Protocol

Cell Research:[5]
- Collapse
  • Cell lines: Human gastric cancer cell lines MKN-28
  • Concentrations: 6 nM
  • Incubation Time: 3 days
  • Method: 2000 cells in 180 μL of medium are seeded in a 96-well plate, and 20 μL of drug solution is simultaneously added in triplicate to each well. The plate is incubated for 3 days at 37°C in a humidified atmosphere of 5% CO2. On day 3, 25 μL of MTT reagent is added to each well. After 4 h of incubation, the medium is removed by aspiration. 0.2 mL of dimethylsulphoxide (DMSO) is added to each well and thoroughly mixed by using a mechanical plate mixer to dissolve the resulting MTT-formazan crystals. Absorbance at 540 nm (OD) is measured by a reader.
    (Only for Reference)
Animal Research:[6]
- Collapse
  • Animal Models: Human colon carcinomas xenografts CX-1
  • Dosages: 33 mg/kg
  • Administration: i.v. every 4 days for 3 injections
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (123.78 mM)
Water Insoluble
Ethanol '53 mg/mL warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
2mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 807.88
Formula

C43H53NO14

CAS No. 114977-28-5
Storage powder
in solvent
Synonyms NSC 628503
Smiles CC1=C2C(C(=O)C3(C(CC4C(C3C(C(C2(C)C)(CC1OC(=O)C(C(C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)O)C)O

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Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05027204 Not yet recruiting Drug: Docetaxel|Drug: Nivolumab Squamous Cell Carcinoma of Head and Neck CSPC ZhongQi Pharmaceutical Technology Co. Ltd. September 2021 Phase 1|Phase 2
NCT04467801 Recruiting Drug: Ipatasertib NSCLC Stage IV|NSCLC Stage IIIB Jun Zhang MD PhD|University of Iowa|University of Kentucky|University of Kansas Medical Center August 18 2021 Phase 2
NCT04811118 Recruiting Drug: Docetaxel for Injection (Albumin-bound)|Drug: Taxotere Advanced Solid Tumors CSPC ZhongQi Pharmaceutical Technology Co. Ltd. May 18 2021 Phase 1
NCT04823910 Not yet recruiting -- Prostate Cancer Physiomics|Portsmouth Hospitals NHS Trust|National Institute for Health Research United Kingdom May 2021 --
NCT04889599 Recruiting Drug: BH009 (Docetaxel injection)|Drug: Docetaxel injection Docetaxel|Solid Tumours|Bioequivalence Zhuhai Beihai Biotech Co. Ltd April 29 2021 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID