Etoposide (依托泊苷）

Etoposide (VP-16; VP-16-213) 是一種常用的抗腫瘤化療劑。Etoposide 抑制拓?fù)洚悩?gòu)酶 II (topoisomerase-II)，從而抑制 DNA 復(fù)制。Etoposide 誘導(dǎo)細(xì)胞周期停滯，凋亡 (apoptosis) 和自噬 (autophagy)。

貨號(hào)：HY-13629
CAS： 33419-42-0

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號(hào)：HY-13629

起訂量：1

規(guī)格:：200mg

價(jià)格:：￥880

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Etoposide (Synonyms: 依托泊苷; VP-16; VP-16-213)

Etoposide (VP-16; VP-16-213) 是一種常用的抗腫瘤化療劑。Etoposide 抑制拓?fù)洚悩?gòu)酶 II (topoisomerase-II)，從而抑制 DNA 復(fù)制。Etoposide 誘導(dǎo)細(xì)胞周期停滯，凋亡 (apoptosis) 和自噬 (autophagy)。

生物活性

Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy^[1].

IC₅₀ & Target^[1]

Topoisomerase II

體外研究(In Vitro)

Etoposide is capable of causing cytotoxicity on pancreatic β-cells by inducing apoptosis through the JNK/ERK-mediated GSK-3 downstream-triggered mitochondria-dependent signaling pathway in RIN-m5F cells^[1].
Etoposide and Anti-Human VEGF significantly abolish P1 sphere-forming ability, an effect associated with apoptosis of this subset of cells^[2].
Etoposide phosphate (0-1μM; 72 hours) inhibits HCT116 FBXW^+/+, FBXW^-/- and p53^-/- as a dose-dependent manner, exhibits IC₅₀s of 0.945 μM; 0.375 μM; and 1.437 μM, respectively^[5].
Etoposide (25 μM; 6 hours) delays p53 recover in FBXW7-deficient cells. In addition, FBXW7 expression is disappeared in FBXW7^-/- cells^[5].

Cell Viability Assay^[5]

Cell Line:	HCT116 FBXW^+/+, FBXW^-/- and p53^-/- cells
Concentration:	0.025 μM, 0.05 μM, 0.075 μM, 0.1 μM, 0.2 μM, 0.4 μM, 0.6 μM, 0.8 μM, 1 μM
Incubation Time:	72 hours
Result:	Inhibits HCT116 FBXW^+/+p>, FBXW^-/- and p53^-/- cell growth as a concentration manner.

體內(nèi)研究(In Vivo)

Etoposide (50 μM) and Anti-Human VEGF-treated hypoxic cells injected intravenously into immunodeficient mice reveals a reduced capacity to induce lung colonies, which also appear with a longer latency period^[2]. Etoposide (10 mg/kg/day, i.v.) with NSC 109724 and NSC 241240, reduces the tumor volume in the hepatoblastoma cell injected NMRI nude mice^[3].

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01032070	OSI Pharmaceuticals\|Astellas Pharma Inc	Recurrent or Refractory Pediatric Ependymoma	September 27, 2010	Phase 2
NCT04101357	BioNTech SE	Solid Tumor\|Extensive-stage Small Cell Lung Cancer	June 19, 2020	Phase 1\|Phase 2
NCT00007852	University of Nebraska\|National Cancer Institute (NCI)\|Genentech, Inc.	Lymphoma	September 2000	Phase 2

分子量：588.56

Formula：C₂₉H₃₂O₁₃

CAS 號(hào)：33419-42-0

中文名稱：依托泊苷；臼乙叉苷；足葉乙甙

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

DMSO : ≥ 39 mg/mL (66.26 mM)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.6991 mL	8.4953 mL	16.9906 mL
5 mM	0.3398 mL	1.6991 mL	3.3981 mL
10 mM	0.1699 mL	0.8495 mL	1.6991 mL

*

請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

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

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
2.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
3.

請(qǐng)依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
4.

請(qǐng)依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
5.

請(qǐng)依序添加每種溶劑： 1% DMSO 99% saline
Solubility: ≥ 0.5 mg/mL (0.85 mM); Clear solution

參考文獻(xiàn)

[1]. Lee KI, et al. Etoposide induces pancreatic β-cells cytotoxicity via the JNK/ERK/GSK-3 signaling-mediated mitochondria-dependent apoptosis pathway. Toxicol In Vitro. 2016 Jul 26. pii: S0887-2333(16)30147-3.

[2]. Calvani M, det al. Etoposide-Anti-Human VEGF a new strategy against human melanoma cells expressing stem-like traits. Oncotarget. 2016 Jun 9. doi: 10.18632/oncotarget.9939.

[3]. Fuchs, J., et al. Comparative activity of NSC 119875, NSC 109724, NSC 123127, NSC 241240, and etoposide in heterotransplanted hepatoblastoma. Cancer, 1998. 83(11): p. 2400-7.

[4]. Hande KR, et al. The Importance of Drug Scheduling in Cancer Chemotherapy: Etoposide as an Example. Oncologist. 1996;1(4):234-239.

[5]. Cui D, et al. FBXW7 Confers Radiation Survival by Targeting p53 for Degradation.Cell Rep. 2020 Jan 14;30(2):497-509.e4.

Etoposide (依托泊苷）

Etoposide (VP-16; VP-16-213) 是一種常用的抗腫瘤化療劑。Etoposide 抑制拓?fù)洚悩?gòu)酶 II (topoisomerase-II)，從而抑制 DNA 復(fù)制。Etoposide 誘導(dǎo)細(xì)胞周期停滯，凋亡 (apoptosis) 和自噬 (autophagy)。

貨號(hào)：HY-13629
CAS： 33419-42-0

品牌：MCE

型號(hào)：HY-13629

起訂量：1

規(guī)格:：200mg

價(jià)格:：￥880

15906629305

在線客服

客服一

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產(chǎn)品詳情

Etoposide (Synonyms: 依托泊苷; VP-16; VP-16-213)

Etoposide (VP-16; VP-16-213) 是一種常用的抗腫瘤化療劑。Etoposide 抑制拓?fù)洚悩?gòu)酶 II (topoisomerase-II)，從而抑制 DNA 復(fù)制。Etoposide 誘導(dǎo)細(xì)胞周期停滯，凋亡 (apoptosis) 和自噬 (autophagy)。

生物活性

Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy^[1].

IC₅₀ & Target^[1]

Topoisomerase II

體外研究(In Vitro)

Etoposide is capable of causing cytotoxicity on pancreatic β-cells by inducing apoptosis through the JNK/ERK-mediated GSK-3 downstream-triggered mitochondria-dependent signaling pathway in RIN-m5F cells^[1].
Etoposide and Anti-Human VEGF significantly abolish P1 sphere-forming ability, an effect associated with apoptosis of this subset of cells^[2].
Etoposide phosphate (0-1μM; 72 hours) inhibits HCT116 FBXW^+/+, FBXW^-/- and p53^-/- as a dose-dependent manner, exhibits IC₅₀s of 0.945 μM; 0.375 μM; and 1.437 μM, respectively^[5].
Etoposide (25 μM; 6 hours) delays p53 recover in FBXW7-deficient cells. In addition, FBXW7 expression is disappeared in FBXW7^-/- cells^[5].

Cell Viability Assay^[5]

Cell Line:	HCT116 FBXW^+/+, FBXW^-/- and p53^-/- cells
Concentration:	0.025 μM, 0.05 μM, 0.075 μM, 0.1 μM, 0.2 μM, 0.4 μM, 0.6 μM, 0.8 μM, 1 μM
Incubation Time:	72 hours
Result:	Inhibits HCT116 FBXW^+/+p>, FBXW^-/- and p53^-/- cell growth as a concentration manner.

體內(nèi)研究(In Vivo)

Etoposide (50 μM) and Anti-Human VEGF-treated hypoxic cells injected intravenously into immunodeficient mice reveals a reduced capacity to induce lung colonies, which also appear with a longer latency period^[2]. Etoposide (10 mg/kg/day, i.v.) with NSC 109724 and NSC 241240, reduces the tumor volume in the hepatoblastoma cell injected NMRI nude mice^[3].

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01032070	OSI Pharmaceuticals\|Astellas Pharma Inc	Recurrent or Refractory Pediatric Ependymoma	September 27, 2010	Phase 2
NCT04101357	BioNTech SE	Solid Tumor\|Extensive-stage Small Cell Lung Cancer	June 19, 2020	Phase 1\|Phase 2
NCT00007852	University of Nebraska\|National Cancer Institute (NCI)\|Genentech, Inc.	Lymphoma	September 2000	Phase 2

分子量：588.56

Formula：C₂₉H₃₂O₁₃

CAS 號(hào)：33419-42-0

中文名稱：依托泊苷；臼乙叉苷；足葉乙甙

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

DMSO : ≥ 39 mg/mL (66.26 mM)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.6991 mL	8.4953 mL	16.9906 mL
5 mM	0.3398 mL	1.6991 mL	3.3981 mL
10 mM	0.1699 mL	0.8495 mL	1.6991 mL

*

請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

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

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
2.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
3.

請(qǐng)依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
4.

請(qǐng)依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
5.

請(qǐng)依序添加每種溶劑： 1% DMSO 99% saline
Solubility: ≥ 0.5 mg/mL (0.85 mM); Clear solution