Oxaliplatin 是一种DNA 合成抑制剂。Oxaliplatin 会导致 DNA 交联损伤，阻止 DNA 复制和转录并导致细胞死亡。Oxaliplatin 以时间依赖方式抑制人黑色素瘤细胞系 C32 和 G361，IC50值分别为 0.98 μM 和 0.14 μM。Oxaliplatin 可以诱导细胞自噬 (autophagy)。
| 生物活性 | Oxaliplatin is aDNA synthesisinhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and inducesapoptosis. Oxaliplatin can be used forcancerresearch[1][2][3]. |
| IC50& Target | |
体外研究
(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 IC50of 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].
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. |
Cell Cycle Analysis[1] | Cell Line: | HCCLM3 and Hep3B cells | | Concentration: | 10 μM | | Incubation Time: | 24 hours | | Result: | Increased the percentage of apoptotic cells (17.70% for HCCLM3 cells; 21.19% for Hep3B cells). |
Cell Cycle Analysis[1] | Cell Line: | HCCLM3 cells | | Concentration: | 10 μM | | Incubation Time: | 48 hours | | Result: | Down-regulated the expression of Bcl-2 and Bcl-xL, and increased the expression of Bax. |
|
体内研究
(In Vivo) | Oxaliplatin (5-10 mg/kg; i.p.; for 32 days; nude mice) inhibits tumor growth[1].
| 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 | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: H2O : 2.17 mg/mL(5.46 mM;ultrasonic and warming and heat to 60℃;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) 配制储备液 | 1 mM | 2.5171 mL | 12.5853 mL | 25.1705 mL | | 5 mM | 0.5034 mL | 2.5171 mL | 5.0341 mL | | 10 mM | --- | --- | --- |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 5% w/v Glucose Solution Solubility: 3.33 mg/mL (8.38 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： PBS Solubility: 1.92 mg/mL (4.83 mM); Clear solution; Need ultrasonic and warming and heat to 60℃
*以上所有助溶剂都可在本网站选购。 |
