Docetaxel (多西他賽)

Docetaxel (RP-56976) 是一種微管解聚 (microtubule depolymerization) 抑制劑，其 IC50 值為 0.2 μM。Docetaxel 是紫杉醇的半合成類似物，能減弱 bcl-2 和 bcl-xL 基因表達的影響。Docetaxel 阻滯 G2/M 細胞周期，導致細胞凋亡 (apoptosis)。貨號：HY-B0011，CAS：114977-28-5

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號：HY-B0011

起訂量：1

規(guī)格:：25mg

價格:：￥670

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產(chǎn)品詳情

Docetaxel (Synonyms: 多西他賽）

生物活性

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].

IC₅₀ & Target

Human Endogenous Metabolite

體外研究(In Vitro)

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].

體內(nèi)研究(In Vivo)

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].

分子量：807.88

CAS 號：114977-28-5

中文名稱：多西他賽；多西紫杉醇

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式：

4°C, protect from light

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

溶解性數(shù)據(jù)

In Vitro:

Ethanol : 50 mg/mL (61.89 mM; Need ultrasonic)

DMSO : ≥ 35 mg/mL (43.32 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.2378 mL	6.1890 mL	12.3781 mL
5 mM	0.2476 mL	1.2378 mL	2.4756 mL
10 mM	0.1238 mL	0.6189 mL	1.2378 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5 mg/mL (6.19 mM); Clear solution
2.

請依序添加每種溶劑： 10% EtOH 90% corn oil
Solubility: ≥ 5 mg/mL (6.19 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
4.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
5.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
6.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
7.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
8.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
9.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
10.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
11.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
12.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution

參考文獻

[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 NSC 125973 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.

Docetaxel (多西他賽)

Docetaxel (RP-56976) 是一種微管解聚 (microtubule depolymerization) 抑制劑，其 IC50 值為 0.2 μM。Docetaxel 是紫杉醇的半合成類似物，能減弱 bcl-2 和 bcl-xL 基因表達的影響。Docetaxel 阻滯 G2/M 細胞周期，導致細胞凋亡 (apoptosis)。貨號：HY-B0011，CAS：114977-28-5

品牌：MCE

型號：HY-B0011

起訂量：1

規(guī)格:：25mg

價格:：￥670

15906629305

在線客服

客服一

產(chǎn)品詳情

Docetaxel (Synonyms: 多西他賽）

生物活性

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].

IC₅₀ & Target

Human Endogenous Metabolite

體外研究(In Vitro)

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].

體內(nèi)研究(In Vivo)

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].

分子量：807.88

CAS 號：114977-28-5

中文名稱：多西他賽；多西紫杉醇

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式：

4°C, protect from light

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

溶解性數(shù)據(jù)

In Vitro:

Ethanol : 50 mg/mL (61.89 mM; Need ultrasonic)

DMSO : ≥ 35 mg/mL (43.32 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.2378 mL	6.1890 mL	12.3781 mL
5 mM	0.2476 mL	1.2378 mL	2.4756 mL
10 mM	0.1238 mL	0.6189 mL	1.2378 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5 mg/mL (6.19 mM); Clear solution
2.

請依序添加每種溶劑： 10% EtOH 90% corn oil
Solubility: ≥ 5 mg/mL (6.19 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
4.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
5.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
6.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
7.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
8.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
9.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
10.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
11.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution
12.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.57 mM); Clear solution

參考文獻

[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 NSC 125973 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.

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Docetaxel (Synonyms: 多西他賽）

Docetaxel (多西他賽)

分享到微信

Docetaxel (Synonyms: 多西他賽）