Docetaxel (RP56976)

For research use only. Not for use in humans.

製品コードS1148 別名:NSC 628503

Docetaxel (RP56976)化学構造

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.

サイズ 価格(税別)  
10mM (1mL in DMSO) JPY 17100
JPY 13600
JPY 46800
JPY 108100
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バルク問合せ

文献中Selleckの製品使用例(125)

製品安全説明書

Microtubule Associated阻害剤の選択性比較

生物活性

製品説明 Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.
ターゲット
Microtubules [1]
(Cell-free assay)
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HSC-3 NYXidnc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPoTWM2OD1yLkCwNFE{OiEQvF2= NHe5bpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6Oi9pPmPBUmdGWjxxYU6=
5637 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTBwMECwNVQ{KM7:TR?= M3PL[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFkzNyd-U1HOS2VTRC:jPh?=
HT-144 NGXJOlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTvcIpzUUN3ME2wMlAxODF3NzFOwG0> NX7H[Y9tRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTJxJ{7TRW5ITVJ:L3G+
NCI-H292 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTHSIZKSzVyPUCuNFAxOTV7IN88US=> NF;CRm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6Oi9pPmPBUmdGWjxxYU6=
HCE-T NXnvZW1WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jVOGlEPTB;MD6wNFAyPjJizszN M1LlRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFkzNyd-U1HOS2VTRC:jPh?=
ESS-1 M{\ZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXlTWM2OD1yLkCwNFE4QSEQvF2= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5Nk8oRlODTlfFVlww[T5?
D-566MG MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvuTWM2OD1yLkCwNFE5OiEQvF2= M{XycFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFkzNyd-U1HOS2VTRC:jPh?=
CAL-62 NVnUNHk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjLbmFGUUN3ME2wMlAxODF6NTFOwG0> NF;FSJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6Oi9pPmPBUmdGWjxxYU6=
GT3TKB NU[yWpVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYWwN5ZWUUN3ME2wMlAxODJ|MjFOwG0> Mo\MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVIwLz6VQV7HSXI9N2F-
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BFTC-905 Mn6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjsSZdYUUN3ME2wMlAxODJ4ODFOwG0> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5Nk8oRlODTlfFVlww[T5?
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HuO-3N1 NV;0O5UzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XUNWlEPTB;MD6wNFA{ODJizszN NHLIXVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6Oi9pPmPBUmdGWjxxYU6=
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CAL-27 NHTUUnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;WcGlEPTB;MD6wNFA{OzlizszN Ml;YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVIwLz6VQV7HSXI9N2F-
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VA-ES-BJ MnTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HFdGlEPTB;MD6wNFA{PzVizszN NILyVm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6Oi9pPmPBUmdGWjxxYU6=
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COLO-800 Mn3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwMECwN|g5KM7:TR?= M2\pflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFkzNyd-U1HOS2VTRC:jPh?=
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GAMG NVO3dm9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwMECwOFE3KM7:TR?= NXHMelhMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTJxJ{7TRW5ITVJ:L3G+
Ca9-22 Mn3SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTBwMECwOFI{KM7:TR?= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5Nk8oRlODTlfFVlww[T5?
SBC-1 M3r5emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTBwMECwOFMh|ryP MoDRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVIwLz6VQV7HSXI9N2F-
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他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
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
体内試験 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]

お薦めの試験操作(参考用のみ)

細胞試験: [5]
- 合併
  • 細胞株: Human gastric cancer cell lines MKN-28
  • 濃度: 6 nM
  • 反応時間: 3 days
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[6]
- 合併
  • 動物モデル: Human colon carcinomas xenografts CX-1
  • 投薬量: 33 mg/kg
  • 投与方法: i.v. every 4 days for 3 injections
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (123.78 mM)
Water Insoluble
Ethanol '53 mg/mL warmed '53
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
2mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 807.88
化学式

C43H53NO14

CAS No. 114977-28-5
Storage powder
in solvent
別名 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

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04823910 Not yet recruiting -- Prostate Cancer Physiomics|Portsmouth Hospitals NHS Trust|National Institute for Health Research United Kingdom May 2021 --
NCT04811118 Not yet recruiting Drug: Docetaxel for Injection (Albumin-bound)|Drug: Taxotere Advanced Solid Tumors CSPC ZhongQi Pharmaceutical Technology Co. Ltd. March 2021 Phase 1
NCT04721015 Recruiting Drug: ABBV-637|Drug: Docetaxel Advanced Solid Tumors Cancer|Non Small Cell Lung Cancer (NSCLC) AbbVie February 18 2021 Phase 1
NCT04656652 Recruiting Drug: DS-1062a|Drug: Docetaxel Non-small Cell Lung Cancer Daiichi Sankyo Inc.|AstraZeneca December 21 2020 Phase 3
NCT04810208 Recruiting Drug: Docetaxel Solid Tumor Lidds AB February 28 2019 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

Microtubule Associatedシグナル伝達経路

相関Microtubule Associated製品

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID