Cabazitaxel
Cabazitaxel(XRP6258; RPR-116258A) is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.
- 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
|
Cell lines |
P-glycoprotein-expressing cell lines with chemotherapy resistance |
|
Preparation method |
The solubility of this compound in DMSO is > 22.3 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
96 hrs |
|
Applications |
Cabazitaxel showed antiproliferative activity by decreasing the lag time of tubulin assembly and the rate of cold-induced microtubule depolymerization. In P-glycoprotein-expressing cell lines with resistance to taxanes (P388/TXT, Calc18/TXT and HL60/TAX) or to other chemotherapy agents (P388/DOX, P388/VCR and KBV1), Cabazitaxel was more effective than Docetaxel (IC50 ranges: Cabazitaxel, 0.013 ~ 0.414 mM; Docetaxel, 0.17 ~ 4.01 mM). Cabazitaxel showed relatively lower resistance factors (2 ~ 10) that those of Docetaxel (5 ~ 59). |
| Animal experiment [1]: | |
|
Animal models |
Mice bearing Docetaxel-sensitive MA16/C adenocarcinomas |
|
Dosage form |
64.5, 40, 24.8 or 15.4 mg/kg; i.v. |
|
Applications |
In mice bearing Docetaxel-sensitive MA16/C adenocarcinomas, Cabazitaxel showed significant anti-tumor activity, inducing CRs in 80% of mice and displaying a log cell kill of 3.7 at the HNTD of 40 mg/kg. The maximum drug concentration in tumors was reached 15 mins after dosing. At 48 hrs after dosing, the concentration of Cabazitaxel in tumors was 40-fold higher than that in plasma. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
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. |
|
Quality Control & MSDS
- View current batch:
Chemical structure
Related Biological Data
Related Biological Data
Related Biological Data
