Cabazitaxel (Synonyms: TXD 258, XRP 6258) |
| Catalog No.GC11765 |
Le cabazitaxel est un dérivé semi-synthétique du taxoÏde naturel 10-désacétylbaccatine III avec une activité antinéoplasique potentielle.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 183133-96-2
Sample solution is provided at 25 µL, 10mM.
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Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.
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].
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:
[1]. Tai X, et al. Cabazitaxel and indocyanine green co-delivery tumor-targeting nanoparticle for improved antitumor efficacy and minimized drug toxicity. J Drug Target. 2016 Sep 9:1-29.
[2]. Gdowski AS, et al. Bone-targeted cabazitaxel nanoparticles for metastatic prostate cancer skeletal lesions and pain. Nanomedicine (Lond). 2017 Sep;12(17):2083-2095.
| Cell experiment [1]: | |
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Cell lines |
P-glycoprotein-expressing cell lines with chemotherapy resistance |
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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. |
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Reacting condition |
96 hrs |
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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]: | |
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Animal models |
Mice bearing Docetaxel-sensitive MA16/C adenocarcinomas |
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Dosage form |
64.5, 40, 24.8 or 15.4 mg/kg; i.v. |
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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. |
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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. |
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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. | |
| Cas No. | 183133-96-2 | SDF | |
| Synonymes | TXD 258, XRP 6258 | ||
| 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 | ||
| Formula | C45H57NO14 | M.Wt | 835.93 |
| Solubility | ≥ 22.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1963 mL | 5.9814 mL | 11.9627 mL |
| 5 mM | 239.3 μL | 1.1963 mL | 2.3925 mL |
| 10 mM | 119.6 μL | 598.1 μL | 1.1963 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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