CabazitaxelCAS# 183133-96-2 |
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Quality Control & MSDS
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| Cas No. | 183133-96-2 | SDF | Download SDF |
| PubChem ID | 9854073 | Appearance | Powder |
| Formula | C45H57NO14 | M.Wt | 835.93 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | XRP6258; RPR-116258A; taxoid XRP6258 | ||
| Solubility | DMSO : ≥ 100 mg/mL (119.63 mM) *"≥" means soluble, but saturation unknown. | ||
| SMILES | CC1=C2C(C(=O)C3(C(CC4C(C3C(C(C2(C)C)(CC1OC(=O)C(C(C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)OC)C)OC | ||
| Standard InChIKey | BMQGVNUXMIRLCK-OAGWZNDDSA-N | ||
| Standard InChI | InChI=1S/C45H57NO14/c1-24-28(57-39(51)33(48)32(26-17-13-11-14-18-26)46-40(52)60-41(3,4)5)22-45(53)37(58-38(50)27-19-15-12-16-20-27)35-43(8,36(49)34(55-10)31(24)42(45,6)7)29(54-9)21-30-44(35,23-56-30)59-25(2)47/h11-20,28-30,32-35,37,48,53H,21-23H2,1-10H3,(H,46,52)/t28-,29-,30+,32-,33+,34+,35-,37-,43+,44-,45+/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.In Vitro:The cytotoxicity of cabazitaxel (100 μg/mL) on 4T1 cells without irradiation is 70.8%. Cabazitaxel (100 μg/mL) exhibits a concentration-dependent antiproliferation effect, with the antiproliferative activity of 56.2%[1].In Vivo:Cabazitaxel (10 mg/kg, i.v.) has certain toxicity to liver and kidney but it can be avoided by integrated into Ans. The body weights of mice treated with AN-ICG-CBX and AN-CBX have a slightly decrease, while body weights of the free CBX group significantly decrease compared to the control group[1]. References: | |||||
Cabazitaxel Dilution Calculator
Cabazitaxel Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.1963 mL | 5.9814 mL | 11.9627 mL | 23.9254 mL | 29.9068 mL |
| 5 mM | 0.2393 mL | 1.1963 mL | 2.3925 mL | 4.7851 mL | 5.9814 mL |
| 10 mM | 0.1196 mL | 0.5981 mL | 1.1963 mL | 2.3925 mL | 2.9907 mL |
| 50 mM | 0.0239 mL | 0.1196 mL | 0.2393 mL | 0.4785 mL | 0.5981 mL |
| 100 mM | 0.012 mL | 0.0598 mL | 0.1196 mL | 0.2393 mL | 0.2991 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Cabazitaxel(XRP6258; RPR-116258A) is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.
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Efficacy of Cabazitaxel Treatment in Metastatic Castration Resistant Prostate Cancer in Second and Later Lines. An Experience from Two German Centers.[Pubmed:28367230]
J Cancer. 2017 Feb 11;8(4):507-512.
Purpose: Several new treatment options for patients with metastatic castration resistant prostate cancer (mCRPC) have been approved within the last years - among them Cabazitaxel (CAB), abiraterone acetate, enzalutamide, and radium-223. The aim of this study was to assess factors predictive for efficacy of CAB. Methods: We analyzed all patients with mCRPC treated with CAB at our institutions between 2011 and 2016. Data were retrieved retrospectively from the electronical patient chart. Results: 69 patients received CAB (26.1% 2(nd) line, 36.2% 3(rd) line, 37.3% >3(rd) line). Median overall survival (OS) on CAB was 10.0 months (95%CI 7.1-12.9). Median progression free survival (PFS) on CAB was 3.9 months (95%CI 3.0-4.8). There were no differences in OS and PFS regarding treatment line of CAB (2(nd) vs. higher; 2(nd)/3(rd) vs. higher). Duration of remission on 1(st) line treatment (> 6 months vs.
Budgetary Impact of Cabazitaxel Use After Docetaxel Treatment for Metastatic Castration-Resistant Prostate Cancer.[Pubmed:28345444]
J Manag Care Spec Pharm. 2017 Apr;23(4):416-426.
BACKGROUND: With the approval of several new treatments for metastatic castration-resistant prostate cancer (mCRPC), budgetary impact is a concern for health plan decision makers. Budget impact models (BIMs) are becoming a requirement in many countries as part of formulary approval or reimbursement decisions. Cabazitaxel is a second-generation taxane developed to overcome resistance to docetaxel and is approved for the treatment of patients with mCRPC previously treated with a docetaxel-containing regimen. OBJECTIVE: To estimate a 1-year projected budget impact of varying utilization rates of Cabazitaxel as a second-line treatment for mCRPC following docetaxel, using a hypothetical U.S. private managed care plan with 1 million members. METHODS: A BIM was developed to evaluate costs for currently available treatment options for patients with mCRPC previously treated with docetaxel. Treatments included in the model were Cabazitaxel, abiraterone acetate, enzalutamide, and radium-223, with utilization rates derived from market research data. Medication costs were calculated according to published pricing benchmarks factored by dosing and duration of therapy as stated in the prescribing information for each agent. Published rates and costs of grade 3-4 adverse events were also factored into the model. In addition, the model reports budget impact under 2 scenarios. In the first base-case scenario, patient out-of-pocket costs were subtracted from the total cost of treatment. In the second scenario, all treatment costs were assumed to be paid by the plan. RESULTS: In a hypothetical 1 million-member health plan population, 100 patients were estimated to receive second-line treatment for mCRPC after treatment with docetaxel. Using current utilization rates for the 4 agents of interest, the base-case scenario estimated the cost of second-line treatment after docetaxel to be $6,331,704, or $0.528 per member per month (PMPM). In a scenario where Cabazitaxel use increases from the base-rate case of 24% to a hypothetical rate of 33%, the PMPM cost would decrease to $0.524, reflecting a cost saving of $0.004 PMPM and equating to incremental savings of $49,546, or $497 per patient per year (PPPY). In the second scenario, when out-of-pocket costs were not considered, the cost of second-line treatment after docetaxel was estimated as $6,733,594, or $0.561 PMPM. With a hypothetical increase in Cabazitaxel use (24%-33%), the PMPM cost would decrease to $0.554, reflecting savings of $0.007 PMPM and equating to incremental savings of $86,136, or $864 PPPY. The primary driver of cost savings with increased Cabazitaxel use was lower acquisition cost. One-way sensitivity analyses revealed that the model results were robust over a wide range of input values (utilization, prevalence, and population parameters). CONCLUSIONS: In the presented BIM, an increase in Cabazitaxel use is expected to result in modest cost savings to the health plan. Patient coinsurance savings may also be realized based on applicable Medicare Part B and Part D calculations. This BIM presents an objective, comprehensive, robust, and user-adaptable tool that health plans and medical decision makers may use to evaluate potential economic impact of formulary and reimbursement decisions. DISCLOSURES: Research and analysis were funded by Sanofi US. The sponsor had the opportunity to review the final draft; however, the authors were responsible for all content and editorial decisions. Flannery, Drea, Hudspeth, and Miao are employees of Sanofi. Miao is an owner of stock in Sanofi. Corman, Gao, and Xue are employees of Pharmerit International and served as consultants to Sanofi during this study. All authors contributed to study design and data collection and analysis. The manuscript was written by Flannery, along with the other authors, and revised by all the authors.
Safety and efficacy of 2-weekly cabazitaxel in metastatic castration-resistant prostate cancer.[Pubmed:28370882]
BJU Int. 2018 Feb;121(2):203-208.
OBJECTIVES: To evaluate the safety and efficacy of a 2-weekly Cabazitaxel schedule in patients with metastatic castration-resistant prostate cancer (mCRPC). MATERIALS AND METHODS: During the period October 2013 to February 2016, 43 patients with mCRPC were treated with Cabazitaxel (16 mg/m(2) , on days 1 and 15 of a 4-week cycle) together with prophylactic granulocyte colony-stimulating factor (G-CSF). The safety profile and efficacy (prostate-specific antigen [PSA] response; biological, clinical or radiological progression-free survival [PFS] and overall survival [OS]) of the treatment were analysed. RESULTS: All patients had received prior docetaxel and 79.1% abiraterone acetate. At inclusion, 46.5% were aged >70 years and 27.9% had an Eastern Cooperative Oncology Group performance status >/=2. Six patients stopped treatment because of toxicity. Grade >/=3 toxicities were: asthenia (16.3%); neutropenia (11.6%); thrombocytopenia (9.3%); diarrhoea (7%), anaemia (4.7%), febrile neutropenia (4.7%) and haematuria (2.3%). In all, 52.4% achieved a >/=30% PSA response and 40.5% had a >/=50% PSA response. The median OS was 15.2 months. CONCLUSION: This prospective pilot study suggests that Cabazitaxel 16 mg/m(2) given 2-weekly has a manageable toxicity profile in docetaxel- and abiraterone acetate-pretreated patients with mCRPC. A prospective phase III trial comparing this regimen with the standard Cabazitaxel regimen is planned to confirm these results.
Synthesis and Characterization of Water-soluble Conjugates of Cabazitaxel Hemiesters-Dextran.[Pubmed:28270079]
Anticancer Agents Med Chem. 2017 Nov 24;17(11):1555-1562.
BACKGROUND: Cabazitaxel (CTX) is a second- generation taxane derivative, a class of potent anticancer drugs with very low water solubility. CTX is used in patients with resistant prostate cancer unresponsive to the first generation taxane, docetaxel. Currently marketed formulations of CTX contain high concentrations of surfactant and ethanol, which cause severe hypersensitivity reactions in patients. METHODS: In order to increase its solubility, two hemiester analogs; CTX-succinate and CTX-glutarate were synthesized and characterized. To improve the solubility of hemiesters even more, dextran as a biocompatible polymer was also conjugated to hemiester analogs. MTT assay was performed on MCF-7 cell line to evaluate the cytotoxicity effect of hemiesters and conjugates. RESULTS: Based on the results, hemiester analogs increased water solubility of the drug up to about 3 and 8 fold. Conjugation to dextran enhanced the CTX solubility to more than 1500 fold. These conjugates released the conjugated CTX in less than 24 hours in a pH dependent manner and showed proper hemocompatibility characteristics. The hemiesters had approximately similar cytotoxicity in comparison with CTX and the dextran conjugates showed higher cytotoxicity effect on MCF-7 cell line.
