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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)。
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 Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT00268333 | GERCOR - Multidisciplinary Oncology Cooperative Group|National Cancer Institute (NCI) | August 2005 | Phase 2 | |
NCT00686166 | Southwest Oncology Group|National Cancer Institute (NCI) | February 2009 | Phase 2 | |
NCT00112658 | UNICANCER | November 2004 | Phase 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)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.5171 mL | 12.5853 mL | 25.1705 mL |
5 mM | 0.5034 mL | 2.5171 mL | 5.0341 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。
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
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)
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 Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT00268333 | GERCOR - Multidisciplinary Oncology Cooperative Group|National Cancer Institute (NCI) | August 2005 | Phase 2 | |
NCT00686166 | Southwest Oncology Group|National Cancer Institute (NCI) | February 2009 | Phase 2 | |
NCT00112658 | UNICANCER | November 2004 | Phase 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)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.5171 mL | 12.5853 mL | 25.1705 mL |
5 mM | 0.5034 mL | 2.5171 mL | 5.0341 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。
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
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)