Cabazitaxel
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
- 1. Sarah D. Burnett, Alexander D. Blanchette, et al. "Cardiotoxicity Hazard and Risk Characterization of ToxCast Chemicals Using Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes from Multiple Donors." Chem Res Toxicol. 2021 Sep 20;34(9):2110-2124. PMID:34448577
- 2. Choi B, Jung H, et al. "Sequential MR Image-Guided Local Immune Checkpoint Blockade Cancer Immunotherapy Using Ferumoxytol Capped Ultralarge Pore Mesoporous Silica Carriers after Standard Chemotherapy." Small. 2019 Nov 7:e1904378. PMID:31697036
- 3. Su F, Ahn S, et al. "Adipose stromal cell targeting suppresses prostate cancer epithelial-mesenchymal transition and chemoresistance." Oncogene. 2018 Oct 25. PMID:30361686
- 4. Blanchette AD, Grimm FA, et al. "Thorough QT/QTc in a Dish: An In Vitro Human Model That Accurately Predicts Clinical Concentration-QTc Relationships." Clin Pharmacol Ther. 2018 Oct 22. PMID:30346629
- 5. Oblad RV, Doughty H, et al. "Application of Mixture Design Response Surface Methodology for Combination Chemotherapy in PC-3 Human Prostate Cancer Cells." Mol Pharmacol. 2018 Jun 8. pii: mol.117.111450. PMID:29884690
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 835.93 |
| Cas No. | 183133-96-2 |
| Formula | C45H57NO14 |
| Solubility | ≥22.3 mg/mL in DMSO; insoluble in H2O; ≥26.6 mg/mL in EtOH |
| SDF | Download SDF |
| Canonical SMILES | CO[C@H]1C[C@]2([H])[C@](CO2)(OC(C)=O)[C@]3([H])[C@]1(C)C([C@H](OC)C4=C(C)[C@@H](OC([C@H](O)[C@H](C5=CC=CC=C5)NC(OC(C)(C)C)=O)=O)C[C@]([C@H]3OC(C6=CC=CC=C6)=O)(O)C4(C)C)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
表达P-糖蛋白的耐药细胞系 |
|
制备方法 |
在DMSO中的溶解度大于22.3 mg/mL。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
|
反应条件 |
96小时 |
|
实验结果 |
Cabazitaxel缩短微管蛋白组装的滞后时间并降低低温诱导的微管解聚速率，具有抗增殖活性。在表达P-糖蛋白的耐紫杉烷细胞系（P388/TXT、Calc18/TXT和HL60/TAX）或耐其它化疗药物细胞系（P388/DOX、P388/VCR和KBV1）中，相对于Docetaxel，Cabazitaxel显示出更显著的作用（IC50范围：Cabazitaxel，0.013 ~ 0.414 mM；Docetaxel，0.17 ~ 4.01 mM）。相对于Docetaxel (5 ~ 59)，Cabazitaxel具有较低的耐药因子 (2 ~ 10)。 |
| 动物实验 [1]: | |
|
动物模型 |
携带对Docetaxel敏感的MA16/C腺癌的小鼠 |
|
给药剂量 |
64.5、40、24.8或15.4 mg/kg；静脉注射 |
|
实验结果 |
在携带对Docetaxel敏感的MA16/C腺癌的小鼠中，Cabazitaxel显示出显著的抗肿瘤活性。在40 mg/kg的HNTD下，80%的小鼠出现CRs，细胞死亡数目的对数值达3.7。给药后15分钟，Cabazitaxel于肿瘤内达最大药物浓度。给药48小时后，Cabazitaxel于肿瘤内的浓度比其在血浆中的浓度高出40倍。 |
|
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1]. Vrignaud P, Sémiond D, Lejeune P, Bouchard H, Calvet L, Combeau C, Riou JF, Commeron A, Lavelle F, Bissery MC. Preclinical antitumor activity of cabazitaxel, a semisynthetic taxane active in taxane-resistant tumors. Clin Cancer Res. 2013 Jun 1;19(11):2973-83. |
|
质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
相关生物数据
