| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
The primary target of Cabazitaxel-d6, like its non-deuterated form, is the microtubule network. It binds to β-tubulin, promoting the assembly of tubulin dimers into stable microtubules and inhibiting their depolymerization. This prevents cell division and leads to cell cycle arrest and apoptosis in rapidly dividing cancer cells. The deuterium atoms do not alter the pharmacological activity but allow for sensitive detection.
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|---|---|
| ln Vitro |
Drug compounds have been modified to include stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to impact a drug's pharmacokinetic and metabolic characteristics, deuteration has drawn attention[1].
In vitro, Cabazitaxel-d6 exhibits the same antiproliferative activity as cabazitaxel against various cancer cell lines, including docetaxel-resistant cells. It has been shown to have higher affinity for β-tubulin isoforms and better brain penetration. However, as an analytical standard, its primary use is not for biological activity assays but for quantification in pharmacokinetic studies. |
| ln Vivo |
In accompanying models, Cabazitaxel is noted to have significant antitumor activity. In murine tumor xenografts (colon C38 and pancreas P03), Cabazitaxel elicites complete tumor regressions. Using SF-295 and U251 human glioblastoma cell lines, both orthotopic and subcutaneous murine xenografts are generated. Cabazitaxel treatment leads to complete regression in the majority of subcutaneously implanted tumors. Furthermore, in orthotopic models, Cabazitaxel leads to complete tumor regression in 4 out of 10 U251 tumors.
In vivo, Cabazitaxel-d6 is used in pharmacokinetic studies to measure the concentration of cabazitaxel in plasma and tissues. Its deuterated nature provides a distinct mass shift, allowing it to be distinguished from endogenous or administered cabazitaxel. It is used as a stable isotope-labeled internal standard to improve the accuracy and precision of LC-MS/MS assays. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies are not typically performed with the deuterated form. However, its binding affinity to tubulin can be studied if needed, though it is assumed to be identical to cabazitaxel. For analytical purposes, the compound's purity and mass spectrometric properties are the primary focus.
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| Cell Assay |
In vitro cell-based assays are not relevant for this product, as it is an analytical standard. However, if one were to test it, it would show the same cytotoxicity as cabazitaxel. The deuterium label does not affect cellular uptake or activity, but it is not used for such purposes.
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| Animal Protocol |
Murine tumor xenografts
In vivo animal studies are also not conducted with the deuterated compound as a therapeutic. Instead, it is used in pharmacokinetic studies where animals are administered cabazitaxel, and the internal standard is added to biological samples for quantification. The compound is not administered to animals itself. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of cabazitaxel, for which this standard is used, include high plasma protein binding, extensive hepatic metabolism, and biliary excretion. The deuterated standard behaves identically in LC-MS, allowing for accurate measurement of cabazitaxel concentrations. It is stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
The toxicity profile of cabazitaxel includes myelosuppression, hypersensitivity reactions, and gastrointestinal side effects. The deuterated standard is used in trace amounts and does not pose a toxicological risk. Standard laboratory safety precautions apply.
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| References |
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| Additional Infomation |
Additional information: Cabazitaxel-d6 is the deuterated version of cabazitaxel, with six deuterium atoms replacing hydrogen atoms at specific positions. It is used as an internal standard for pharmacokinetic studies. This product is for research use only and is not intended for therapeutic or diagnostic use.
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| Molecular Formula |
C45H57NO14
|
|---|---|
| Molecular Weight |
835.932394742966
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| Exact Mass |
841.415
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| CAS # |
1383561-29-2
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| Related CAS # |
Cabazitaxel;183133-96-2;Cabazitaxel-d9;1383572-19-7
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| PubChem CID |
57524246
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| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
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| Boiling Point |
870.7±65.0 °C at 760 mmHg
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| Flash Point |
480.4±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.592
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| LogP |
7.55
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
60
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| Complexity |
1690
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| Defined Atom Stereocenter Count |
11
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| SMILES |
[2H]C([2H])([2H])O[C@H]1C[C@@H]2[C@@](CO2)([C@@H]3[C@@]1(C(=O)[C@@H](C4=C([C@H](C[C@@]([C@H]3OC(=O)C5=CC=CC=C5)(C4(C)C)O)OC(=O)[C@@H]([C@H](C6=CC=CC=C6)NC(=O)OC(C)(C)C)O)C)OC([2H])([2H])[2H])C)OC(=O)C
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| InChi Key |
BMQGVNUXMIRLCK-YHVGWTKXSA-N
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| InChi Code |
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/i9D3,10D3
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| Chemical Name |
[(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-acetyloxy-1-hydroxy-15-[(2R,3S)-2-hydroxy-3-[(2-methylpropan-2-yl)oxycarbonylamino]-3-phenylpropanoyl]oxy-10,14,17,17-tetramethyl-11-oxo-9,12-bis(trideuteriomethoxy)-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl] benzoate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1963 mL | 5.9814 mL | 11.9627 mL | |
| 5 mM | 0.2393 mL | 1.1963 mL | 2.3925 mL | |
| 10 mM | 0.1196 mL | 0.5981 mL | 1.1963 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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