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Oxaliplatin ( 奧沙利鉑)

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Oxaliplatin 是一種 DNA 合成 抑制劑。Oxaliplatin 會(huì)導(dǎo)致 DNA 交聯(lián)損傷,阻止 DNA 復(fù)制和轉(zhuǎn)錄并導(dǎo)致細(xì)胞死亡。Oxaliplatin 以時(shí)間依賴方式抑制人黑色素瘤細(xì)胞系 C32 和 G361,IC50 值分別為 0.98 μM 和 0.14 μM。Oxaliplatin 可以誘導(dǎo)細(xì)胞自噬 (autophagy)。 貨號(hào):HY-17371
參數(shù)品牌:MCE
產(chǎn)品參數(shù)
品牌:MCE
型號(hào):HY-17371
起訂量:1
規(guī)格::50mg
價(jià)格::¥550
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產(chǎn)品詳情

Oxaliplatin ( 奧沙利鉑)

Oxaliplatin 是一種 DNA 合成 抑制劑。Oxaliplatin 會(huì)導(dǎo)致 DNA 交聯(lián)損傷,阻止 DNA 復(fù)制和轉(zhuǎn)錄并導(dǎo)致細(xì)胞死亡。Oxaliplatin 以時(shí)間依賴方式抑制人黑色素瘤細(xì)胞系 C32 和 G361,IC50 值分別為 0.98 μM 和 0.14 μM。Oxaliplatin 可以誘導(dǎo)細(xì)胞自噬 (autophagy)。

生物活性

Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and induces apoptosis. Oxaliplatin can be used for cancer research[1][2][3].


IC50 & Target

IC50: DNA synthesis[1]


體外研究(In Vitro)

Oxaliplatin (24-72 hours; 2-128 μM; HCC, HCCLM3 and Hep3B cells) inhibits cell growth and induces apoptosis[1].

Oxaliplatin (10 μM; 15-240 mins; CEM cells ) induces primary and secondary DNA lesions, including DNA cross-links (ISC) and DNA-protein cross-links (DPC)[2].
Oxaliplatin (0.01 to 100 μM; 24 hours) potently inhibits bladder carcinoma cell lines RT4 and TCCSUP, ovarian carcinoma cell line A2780, colon carcinoma cell line HT-29, glioblastoma cell lines U-373MG and U-87MG, and melanoma cell lines SK-MEL-2 and HT-144 with IC50 of 11 μM, 15 μM, 0.17 μM, 0.97 μM, 2.95 μM, 17.6 μM, 30.9 μM and 7.85 μM, respectively[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line:HCC, HCCLM3 and Hep3B cells
Concentration:24, 48 and 72 hours
Incubation Time:2, 4, 8, 16, 32, 64 and 128 μM
Result:Decreased cell viability in a dose- and time-dependent manner.


體內(nèi)研究(In Vivo)

Oxaliplatin (5-10 mg/kg; i.p.; for 32 days; nude mice) inhibits tumor growth[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:Nude mice[1]
Dosage:5 and 10 mg/kg
Administration:Intraperitoneal injection; for 32 days
Result:Reduced tumor volume in HCCLM3 tumor xenografts.


Clinical Trial

NCT NumberSponsorConditionStart DatePhase
NCT00268333GERCOR - Multidisciplinary Oncology Cooperative Group|National Cancer Institute (NCI)
Colorectal Cancer
August 2005Phase 2
NCT00686166Southwest Oncology Group|National Cancer Institute (NCI)
Colorectal Cancer
February 2009Phase 2
NCT00112658UNICANCER
Pancreatic Cancer
November 2004Phase 2|Phase 3

分子量:397.29


Formula:C8H14N2O4Pt


CAS 號(hào):61825-94-3


中文名稱:奧沙利鉑


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)


H2O : 2.17 mg/mL (5.46 mM; ultrasonic and warming and heat to 60°C; DMSO can inactivate Oxaliplatin's activity)

DMF : 1.67 mg/mL (4.20 mM; Need ultrasonic; DMSO can inactivate Oxaliplatin's activity)

Ethanol : < 1 mg/mL (insoluble; DMSO can inactivate Oxaliplatin's activity)

配制儲(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.5171 mL12.5853 mL25.1705 mL
5 mM0.5034 mL2.5171 mL5.0341 mL
10 mM---------
*

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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 1.


    請(qǐng)依序添加每種溶劑: 5% w/v Glucose Solution

    Solubility: 3.33 mg/mL (8.38 mM); Clear solution; Need ultrasonic

參考文獻(xiàn)

[1]. Raymond E, et al. Oxaliplatin: a review of preclinical and clinical studies. Ann Oncol. 1998 Oct;9(10):1053-71.

[2]. Mohammed MQ, et al. Oxaliplatin is active in vitro against human melanoma cell lines: comparison with NSC 119875 and NSC 241240. Anticancer Drugs. 2000 Nov;11(10):859-63.

[3]. Pendyala L, et al. In vitro cytotoxicity, protein binding, red blood cell partitioning, and biotransformation of oxaliplatin. Cancer Res. 1993 Dec 15;53(24):5970-6.

[4]. Wang Z, et al. Oxaliplatin induces apoptosis in hepatocellular carcinoma cells and inhibits tumor growth. Expert Opin Investig Drugs. 2009 Nov;18(11):1595-604

[5]. Mathé G, et al. Oxalato-platinum or 1-OHP, a third-generation platinum complex: an experimental and clinical appraisal and preliminary comparison with cis-platinum. Biomed Pharmacother. 1989;43(4):237-50.

[6]. Schellingerhout D, et al. Impairment of retrograde neuronal transport in oxaliplatin-induced neuropathy demonstrated by molecular imaging. PLoS One. 2012;7(9):e45776. doi: 10.1371/journal.pone.0045776. Epub 2012 Sep 20.

[7]. Park GY, et al. Phenanthriplatin, a monofunctional DNA-binding platinum anticancer drug candidate with unusual potency and cellular activity profile. Proc Natl Acad Sci U S A. 2012 Jul 24;109(30):11987-92.

[8]. Yi Yao, et al. Comparative proteomic analysis of colon cancer cells in response to oxaliplatin treatment. Biochim Biophys Acta. 2009 Oct;1794(10):1433-40.

[9]. Garrett MJ, et, al. Capecitabine, Oxaliplatin, and Bevacizumab (BCapOx) Regimen for Metastatic Colorectal Cancer. Hosp Pharm. 2017 May;52(5):341-347.


Oxaliplatin ( 奧沙利鉑)
Oxaliplatin ( 奧沙利鉑)

Oxaliplatin ( 奧沙利鉑)

分享到微信

×
Oxaliplatin 是一種 DNA 合成 抑制劑。Oxaliplatin 會(huì)導(dǎo)致 DNA 交聯(lián)損傷,阻止 DNA 復(fù)制和轉(zhuǎn)錄并導(dǎo)致細(xì)胞死亡。Oxaliplatin 以時(shí)間依賴方式抑制人黑色素瘤細(xì)胞系 C32 和 G361,IC50 值分別為 0.98 μM 和 0.14 μM。Oxaliplatin 可以誘導(dǎo)細(xì)胞自噬 (autophagy)。 貨號(hào):HY-17371
品牌:MCE
型號(hào):HY-17371
起訂量:1
規(guī)格::50mg
價(jià)格::¥550
15906629305
在線客服
產(chǎn)品詳情

Oxaliplatin ( 奧沙利鉑)

Oxaliplatin 是一種 DNA 合成 抑制劑。Oxaliplatin 會(huì)導(dǎo)致 DNA 交聯(lián)損傷,阻止 DNA 復(fù)制和轉(zhuǎn)錄并導(dǎo)致細(xì)胞死亡。Oxaliplatin 以時(shí)間依賴方式抑制人黑色素瘤細(xì)胞系 C32 和 G361,IC50 值分別為 0.98 μM 和 0.14 μM。Oxaliplatin 可以誘導(dǎo)細(xì)胞自噬 (autophagy)。

生物活性

Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and induces apoptosis. Oxaliplatin can be used for cancer research[1][2][3].


IC50 & Target

IC50: DNA synthesis[1]


體外研究(In Vitro)

Oxaliplatin (24-72 hours; 2-128 μM; HCC, HCCLM3 and Hep3B cells) inhibits cell growth and induces apoptosis[1].

Oxaliplatin (10 μM; 15-240 mins; CEM cells ) induces primary and secondary DNA lesions, including DNA cross-links (ISC) and DNA-protein cross-links (DPC)[2].
Oxaliplatin (0.01 to 100 μM; 24 hours) potently inhibits bladder carcinoma cell lines RT4 and TCCSUP, ovarian carcinoma cell line A2780, colon carcinoma cell line HT-29, glioblastoma cell lines U-373MG and U-87MG, and melanoma cell lines SK-MEL-2 and HT-144 with IC50 of 11 μM, 15 μM, 0.17 μM, 0.97 μM, 2.95 μM, 17.6 μM, 30.9 μM and 7.85 μM, respectively[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line:HCC, HCCLM3 and Hep3B cells
Concentration:24, 48 and 72 hours
Incubation Time:2, 4, 8, 16, 32, 64 and 128 μM
Result:Decreased cell viability in a dose- and time-dependent manner.


體內(nèi)研究(In Vivo)

Oxaliplatin (5-10 mg/kg; i.p.; for 32 days; nude mice) inhibits tumor growth[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:Nude mice[1]
Dosage:5 and 10 mg/kg
Administration:Intraperitoneal injection; for 32 days
Result:Reduced tumor volume in HCCLM3 tumor xenografts.


Clinical Trial

NCT NumberSponsorConditionStart DatePhase
NCT00268333GERCOR - Multidisciplinary Oncology Cooperative Group|National Cancer Institute (NCI)
Colorectal Cancer
August 2005Phase 2
NCT00686166Southwest Oncology Group|National Cancer Institute (NCI)
Colorectal Cancer
February 2009Phase 2
NCT00112658UNICANCER
Pancreatic Cancer
November 2004Phase 2|Phase 3

分子量:397.29


Formula:C8H14N2O4Pt


CAS 號(hào):61825-94-3


中文名稱:奧沙利鉑


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)


H2O : 2.17 mg/mL (5.46 mM; ultrasonic and warming and heat to 60°C; DMSO can inactivate Oxaliplatin's activity)

DMF : 1.67 mg/mL (4.20 mM; Need ultrasonic; DMSO can inactivate Oxaliplatin's activity)

Ethanol : < 1 mg/mL (insoluble; DMSO can inactivate Oxaliplatin's activity)

配制儲(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.5171 mL12.5853 mL25.1705 mL
5 mM0.5034 mL2.5171 mL5.0341 mL
10 mM---------
*

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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 1.


    請(qǐng)依序添加每種溶劑: 5% w/v Glucose Solution

    Solubility: 3.33 mg/mL (8.38 mM); Clear solution; Need ultrasonic

參考文獻(xiàn)

[1]. Raymond E, et al. Oxaliplatin: a review of preclinical and clinical studies. Ann Oncol. 1998 Oct;9(10):1053-71.

[2]. Mohammed MQ, et al. Oxaliplatin is active in vitro against human melanoma cell lines: comparison with NSC 119875 and NSC 241240. Anticancer Drugs. 2000 Nov;11(10):859-63.

[3]. Pendyala L, et al. In vitro cytotoxicity, protein binding, red blood cell partitioning, and biotransformation of oxaliplatin. Cancer Res. 1993 Dec 15;53(24):5970-6.

[4]. Wang Z, et al. Oxaliplatin induces apoptosis in hepatocellular carcinoma cells and inhibits tumor growth. Expert Opin Investig Drugs. 2009 Nov;18(11):1595-604

[5]. Mathé G, et al. Oxalato-platinum or 1-OHP, a third-generation platinum complex: an experimental and clinical appraisal and preliminary comparison with cis-platinum. Biomed Pharmacother. 1989;43(4):237-50.

[6]. Schellingerhout D, et al. Impairment of retrograde neuronal transport in oxaliplatin-induced neuropathy demonstrated by molecular imaging. PLoS One. 2012;7(9):e45776. doi: 10.1371/journal.pone.0045776. Epub 2012 Sep 20.

[7]. Park GY, et al. Phenanthriplatin, a monofunctional DNA-binding platinum anticancer drug candidate with unusual potency and cellular activity profile. Proc Natl Acad Sci U S A. 2012 Jul 24;109(30):11987-92.

[8]. Yi Yao, et al. Comparative proteomic analysis of colon cancer cells in response to oxaliplatin treatment. Biochim Biophys Acta. 2009 Oct;1794(10):1433-40.

[9]. Garrett MJ, et, al. Capecitabine, Oxaliplatin, and Bevacizumab (BCapOx) Regimen for Metastatic Colorectal Cancer. Hosp Pharm. 2017 May;52(5):341-347.


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