Carboplatin
(Synonyms: 卡铂; NSC 241240) 目录号 : GC11207
卡铂（Carboplatin；NSC 241240）是一种非特异性DNA交联剂，抑制DNA合成和转录，其主要靶点是DNA，而不是特定的蛋白质。
Cas No.:41575-94-4
Sample solution is provided at 25 µL, 10mM.
Carboplatin (NSC 241240) is a non-specific DNA cross-linking agent that inhibits DNA synthesis and transcription. Its main target is DNA rather than specific proteins[1]. Carboplatin is commonly used in cancer treatment research and is an effective anticancer drug, especially for ovarian cancer, breast cancer, etc. [2]. Platinum drugs are not recommended to be dissolved in DMSO because they are easily inactivated[3].
In vitro, ten ovarian cancer cells were treated with Carboplatin (0-100μM) for 24h, and all showed strong or moderate cell inhibitory activity. Among them, OV2978 and TOV2881EP cells showed strong sensitivity to Carboplatin, with IC50 <1 μM[4]. Carboplatin (0-100μM) treated Brca1 and Brca2 cells for 72h, which significantly reduced cell survival rates, with IC50 of 3.4μM and 1.9μM, respectively[5].
In vivo, carboplatin (25 mg/kg) was intraperitoneally injected into mice inoculated with OVCAR5 tumor cells and significantly inhibited tumor growth[6]. Carboplatin (15 mg/kg) was intraperitoneally injected into NOD-SCID xenograft mice and combined with panobinostat significantly inhibited tumor growth, showing a synergistic anticancer effect[7].
References:
[1] Doshi G, Sonpavde G, Sternberg C N. Clinical and pharmacokinetic evaluation of satraplatin[J]. Expert opinion on drug metabolism & toxicology, 2012, 8(1): 103-111.
[2] Thomadaki H, Scorilas A. Molecular profile of breast versus ovarian cancer cells in response to treatment with the anticancer drugs cisplatin, carboplatin, doxorubicin, etoposide and taxol[J]. 2008.
[3] Hall M D, Telma K A, Chang K E, et al. Say no to DMSO: dimethylsulfoxide inactivates cisplatin, carboplatin, and other platinum complexes[J]. Cancer research, 2014, 74(14): 3913-3922.
[4] Sauriol S A, Simeone K, Portelance L, et al. Modeling the diversity of epithelial ovarian cancer through ten novel well characterized cell lines covering multiple subtypes of the disease[J]. Cancers, 2020, 12(8): 2222.
[5] Clark C C, Weitzel J N, O'Connor T R. Enhancement of synthetic lethality via combinations of ABT-888, a PARP inhibitor, and carboplatin in vitro and in vivo using BRCA1 and BRCA2 isogenic models[J]. Molecular cancer therapeutics, 2012, 11(9): 1948-1958.
[6] Patel M, Wang Y, Bartom E T, et al. The ratio of toxic-to-Nontoxic mirnas predicts platinum sensitivity in ovarian cancer[J]. Cancer research, 2021, 81(15): 3985-4000.
[7] Wang L, Syn N L X, Subhash V V, et al. Pan-HDAC inhibition by panobinostat mediates chemosensitization to carboplatin in non-small cell lung cancer via attenuation of EGFR signaling[J]. Cancer letters, 2018, 417: 152-160.
卡铂（Carboplatin；NSC 241240）是一种非特异性DNA交联剂，抑制DNA合成和转录，其主要靶点是DNA，而不是特定的蛋白质[1]。Carboplatin通常用于癌症治疗研究，是一种有效的抗癌药物，特别是用于卵巢癌、乳腺癌等[2]。铂类药物不建议用DMSO溶解，易失活[3]。
在体外，Carboplatin（0-100μM）处理十种卵巢癌细胞24h，均表现出较强或中等的细胞抑制活性，其中OV2978和TOV2881EP细胞对Carboplatin表现出很强的敏感性，IC50<1 μM[4]。Carboplatin（0-100μM）处理Brca1和Brca2细胞72h，显著降低了细胞存活率，IC50分别为3.4μM、1.9μM[5]。
在体内，Carboplatin（25mg/kg）通过腹腔注射治疗接种OVCAR5肿瘤细胞的小鼠，显著抑制了肿瘤生长[6]。Carboplatin（15mg/kg）通过腹腔注射治疗NOD-SCID异种移植小鼠，与帕比司他（panobinostat）联合使用显著抑制了肿瘤的生长，显示出协同抗癌效果[7]。
| Cell experiment [1]: | |
|
Cell lines |
Ovarian cancer cell lines |
|
Preparation Method |
Cells were incubated with different concentrations (0-100 μM) of carboplatin for 24 h, and then the treatment medium was replaced with fresh complete OSE medium. |
|
Reaction Conditions |
0-100μM; 24h |
|
Applications |
All cell lines tested showed strong or moderate sensitivity to carboplatin. |
| Animal experiment [2]: | |
|
Animal models |
Female athymic nude mice |
|
Preparation Method |
Female athymic nude mice were injected intraperitoneally (i.p.) with 2 million OVCAR5 OC cells to induce tumors. After 2 weeks inoculation mice were treated i.p. with PBS or 25mg/kg carboplatin in the following treatment regimens: once-a-week for 3 weeks; 3-week carboplatin followed by two-week no drug recovery; additional two weeks carboplatin after recovery. Xenograft tumors were collected 1 week after carboplatin treatment and processed for cancer cell isolation and RNA extraction. |
|
Dosage form |
25mg/kg; i.p. |
|
Applications |
OVCAR5 tumors treated with carboplatin were in general smaller compared with those of PBS injected control animals. |
|
References: [1] Sauriol S A, Simeone K, Portelance L, et al. Modeling the diversity of epithelial ovarian cancer through ten novel well characterized cell lines covering multiple subtypes of the disease[J]. Cancers, 2020, 12(8): 2222. [2] Patel M, Wang Y, Bartom E T, et al. The ratio of toxic-to-Nontoxic mirnas predicts platinum sensitivity in ovarian cancer[J]. Cancer research, 2021, 81(15): 3985-4000. |
|
| Cas No. | 41575-94-4 | SDF | |
| 别名 | 卡铂; NSC 241240 | ||
| 化学名 | azane;cyclobutane-1,1-dicarboxylate;platinum(2+) | ||
| Canonical SMILES | C1CC(C1)(C(=O)[O-])C(=O)[O-].N.N.[Pt+2] | ||
| 分子式 | C6H12N2O4Pt | 分子量 | 371.25 |
| 溶解度 | ≥ 10 mg/mL in Water with gentle warming.（DMSO can inactivate Carboplatin's activity） | 储存条件 | 4°C, protect from light |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6936 mL | 13.468 mL | 26.936 mL |
| 5 mM | 0.5387 mL | 2.6936 mL | 5.3872 mL |
| 10 mM | 0.2694 mL | 1.3468 mL | 2.6936 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet