Docetaxel

カタログ番号 T1034 CAS 114977-28-5

別名: NSC 628503, RP-56976

Docetaxel (RP-56976) is a semi-synthetic analog of paclitaxel, a microtubule depolymerization inhibitor (IC50=0.2 μM). Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression and exhibits apoptosis-inducing, anti-tumor activity.

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Docetaxel, CAS 114977-28-5

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
25 mg	在庫あり	￥ 7,000
50 mg	在庫あり	￥ 9,000
100 mg	在庫あり	￥ 13,000
200 mg	在庫あり	￥ 19,000
500 mg	在庫あり	￥ 31,500
1 g	在庫あり	￥ 45,500
1 mL * 10 mM (in DMSO)	在庫あり	￥ 12,000

バルクのお問い合わせ

バッチを選択

純度: 99.29%

COA DATASHEET SDS HNMR HPLC

純度: 99.15%

COA DATASHEET SDS HNMR HPLC

純度: 99.03%

COA DATASHEET SDS HNMR HPLC

純度: 98.92%

COA DATASHEET SDS HNMR HPLC

COA DATASHEET SDS

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	Docetaxel (RP-56976) is a semi-synthetic analog of paclitaxel, a microtubule depolymerization inhibitor (IC50=0.2 μM). Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression and exhibits apoptosis-inducing, anti-tumor activity.
ターゲット＆IC50	Microtubule:0.2 μM
In vitro	METHODS: Human lung cancer cells NCI-H460 were treated with Docetaxel (0.2-200 nmol/L) for 24-72 h, and cell viability was measured by MTS. RESULTS: The IC50 of NCI-H460 to Docetaxel was 0.030 μmol/L at 72 h and 0.116 μmol/L at 24 h. [1] METHODS: Human prostate cancer cells PC-3, DU-145 and LNCaP were treated with Docetaxel (0.5-4 nM) for 48 h. Apoptosis was detected by Flow Cytometry. RESULTS: High-dose Docetaxel treatment significantly increased the proportion of Annexin V+ apoptotic cells. [2]
In vivo	METHODS: To detect anti-tumor activity in vivo, Docetaxel (5-10 mg/kg) and PD-1 inhibitor (200 μg/only) were intraperitoneally injected into CB17 SCID mice carrying mouse prostate cancer tumor RM-1 five times a week for ten days. RESULTS: PD-1 inhibitor combined with Docetaxel had a synergistic effect on prostate cancer in mice, inhibiting the growth of prostate tumors, increasing the survival rate and reducing adverse effects. [3] METHODS: To assay antitumor activity in vivo, Docetaxel (7.5-15 mg/kg, intratumorally injected IT twice weekly for six weeks; or 20-40 mg/kg weekly intravenously injected IV) was administered to C57BL/6 mice harboring HNSCC tumors HN30 or HN12. RESULTS: IT Docetaxel improved overall survival and disease-free survival and reversed tumor growth. At equivalent dose levels, IT Docetaxel resulted in 26-fold higher peak tumor concentrations and 24-fold longer tumor exposure than IV treatment. [4]
細胞研究	NCI-H460 cells (4 × 10^3) were grown in 100 μl of DMEM medium containing serum per well in a 96-well plate. After 24 h, the cells were treated with docetaxel (0, 0.2, 0.63, 2, 6.3, 20, 63 and 200 nmol/L, respectively) for 72 h. Every treatment was triplicate in the same experiment. Then 20 μl of MTS was added to each well for 1 to 4 h at 37°C. After incubation, the absorbance was read at a wavelength of 490 nm according to the manufacturer's protocol. The IC50 calculation was performed with GraphPad Prism 5.0 software [2].
動物実験	Docetaxel (0, 10, 20, 30, 40, 60, and 80 mg/kg per week) was given once a week for 3 weeks for mice. Because more than 30 mg/kg per week of the drug caused body weight loss in mice, 20 mg/kg per week of docetaxel was judged to be the maximum nontoxic dose. Docetaxel (20 mg/kg per week) was 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) was removed, fixed in 20 N Mildform solution (containing 8% formaldehyde in a buffered solution), and embedded in paraffin blocks, and sections of 5 mm were put on glass slides. Apoptosis was detected using the terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) method, using the Apop Tag Peroxidase In Situ Apoptosis Detection Kit. Specimens were dewaxed and immersed in phosphate-buffered saline for 5 minutes at room temperature, incubated with 20 mg/ml proteinase K for 15 minutes at room temperature, and then quenched of endogenous peroxidase in 2% hydrogen peroxide in phosphate-buffered saline. Terminal deoxynucleotidyl transferase enzyme was applied directly onto the specimens, which were then incubated at 37°C for 1 hour. The reaction was terminated by transferring the slides to stop/wash buffer for 10 minutes at room temperature, and then specimens were covered with peroxidase-conjugated anti-digoxigenin antibody and incubated for 30 minutes at room temperature. Specimens were then soaked in staining buffer containing 0.05% diaminobenzidine to achieve color development. Finally, the specimens were counterstained by immersion in Mayer's hematoxylin solution. Apoptotic cells were counted under a light microscope in a good longitudinal crypt section. Starting at the base of the crypt column, the TUNEL-positive cells were counted up to the 18th cell position in each crypt.One hundred crypt sections were scored in each animal, and a frequency of TUNELpositive cells per crypt was calculated. Dosing time-dependent influence of docetaxel on intestinal apoptosis was also examined in female Balb/c mice [5].
植物由来	天然物製品 > ナデシコ科 > ナデシコ属

別名	NSC 628503, RP-56976
分子量	807.88
分子式	C43H53NO14
CAS No.	114977-28-5

保存条件

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

Ethanol: 80.8 mg/mL (100 mM)

DMSO: 60 mg/mL (74.27 mM)

参考文献

1. 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. 2. Yang C, et al. Effect of docetaxel on the regulation of proliferation and apoptosis of human prostate cancer cells. Mol Med Rep. 2019 May;19(5):3864-3870. 3. Zhou S, et al. PD-1 inhibitor combined with Docetaxel exerts synergistic anti-prostate cancer effect in mice by down-regulating the expression of PI3K/AKT/NFKB-P65/PD-L1 signaling pathway. Cancer Biomark. 2024 Jan 17. 4. Yoo GH, et al. An in vivo evaluation of docetaxel delivered intratumorally in head and neck squamous cell carcinoma. Arch Otolaryngol Head Neck Surg. 2005 May;131(5):418-29. 5. 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. 6. Attia RT, et al. The chemomodulatory effects of glufosfamide on docetaxel cytotoxicity in prostate cancer cells. PeerJ. 2016 Jun 29;4:e2168. 7. 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. 8. Chen Y, Li K, Gong D, et al. ACLY: A biomarker of recurrence in breast cancer. Pathology-Research and Practice. 2020: 153076. 9. Dong H, Sun H, Zheng J. A microchip for integrated single-cell genotoxicity assay[J]. Talanta. 2016, 161: 804-811. 10. Li Q, Qin T, Bi Z, et al. Rac1 activates non-oxidative pentose phosphate pathway to induce chemoresistance of breast cancer[J]. Nature Communications. 2020, 11(1): 1-18.

引用文献

1. Li Q, Qin T, Bi Z, et al. Rac1 activates non-oxidative pentose phosphate pathway to induce chemoresistance of breast cancer. Nature Communications. 2020, 11(1): 1-18. 2. Chen Y, Li K, Gong D I, et al. ACLY: A biomarker of recurrence in breast cancer. Pathology-Research and Practice. 2020, 216(9): 153076 3. Wavelet-Vermuse C, Odnokoz O, Xue Y, et al. CDC20-Mediated hnRNPU Ubiquitination Regulates Chromatin Condensation and Anti-Cancer Drug Response. Cancers. 2022, 14(15): 3732. 4. Dong H, Sun H, Zheng J. A microchip for integrated single-cell genotoxicity assay. Talanta. 2016, 161: 804-811. 5. Liu S, Tao Y, Wu S, et al.Sanguinarine chloride induces ferroptosis by regulating ROS/BACH1/HMOX1 signaling pathway in prostate cancer.Chinese Medicine.2024, 19(1): 1-18. 6. Tao Y, Lu J, Li L, et al.Raltitrexed induces apoptosis through activating ROS-mediated ER stress by impeding HSPA8 expression in prostate cancer cells.Biochimica et Biophysica Acta (BBA)-Molecular Cell Research.2024: 119684.

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Docetaxel 114977-28-5 Apoptosis Cytoskeletal Signaling Metabolism Microtubule Associated Endogenous Metabolite NSC628503 inhibit Inhibitor NSC 628503 RP 56976 RP56976 NSC-628503 RP-56976 Microtubule/Tubulin inhibitor

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

Docetaxel

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords