Larotaxel
Based on 1 Customer Validation
Larotaxel (XRP9881) is an orally active and blood-brain barrier penetrant Microtubule stabilizer with an IC50 of 0.21 μM. Larotaxel shows activity in Taxane-resistant tumor models. Larotaxel exhibits antitumor activity in intracranial glioblastoma models. Larotaxel can be used for research on advanced solid tumors.
For research use only. We do not sell to patients.
- Purity : 99.50%
- CAS No.: 156294-36-9
- Formula: C45H53NO14
- Molecular Weight:831.90
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
101.4 nM
Compound: Larotaxel
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Cytotoxicity against human paclitaxl resistant A549 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human paclitaxl resistant A549 cells after 72 hrs by sulforhodamine B assay
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[PMID: 30036834] |
| A549 | IC50 |
12.1 nM
Compound: Larotaxel
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Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay
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[PMID: 30036834] |
| KB | IC50 |
15.8 nM
Compound: Larotaxel
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Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay
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[PMID: 30036834] |
| MCF7 | IC50 |
18.6 nM
Compound: Larotaxel
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Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay
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[PMID: 30036834] |
| NCI/ADR-RES | IC50 |
280.8 nM
Compound: Larotaxel
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Cytotoxicity against human MCF7/ADR cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human MCF7/ADR cells after 72 hrs by sulforhodamine B assay
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[PMID: 30036834] |
In Vitro
Larotaxel stabilizes microtubules in cell-free assays, preventing cold-induced depolymerization with an IC50 of 0.21 μM[1].
Larotaxel shows in vitro activity in various Taxane-resistant tumor models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 156294-36-9
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Appearance Solid
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Molecular Weight 831.90
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Formula C45H53NO14
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Color White to off-white
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SMILES
O=C([C@]1([H])OC(C)=O)[C@@]23[C@@]([C@@H]([C@@]4(O)C(C)(C)C1=C([C@H](OC([C@H](O)[C@H](C5=CC=CC=C5)NC(OC(C)(C)C)=O)=O)C4)C)OC(C6=CC=CC=C6)=O)([H])[C@]7([C@@](OC7)([H])C[C@@H]2C3)OC(C)=O
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Synonyms
XRP9881
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : ≥ 50 mg/mL (60.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (298 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2021 mL | 6.0103 mL | 12.0207 mL | 30.0517 mL |
| 5 mM | 0.2404 mL | 1.2021 mL | 2.4041 mL | 6.0103 mL | |
| 10 mM | 0.1202 mL | 0.6010 mL | 1.2021 mL | 3.0052 mL | |
| 15 mM | 0.0801 mL | 0.4007 mL | 0.8014 mL | 2.0034 mL | |
| 20 mM | 0.0601 mL | 0.3005 mL | 0.6010 mL | 1.5026 mL | |
| 25 mM | 0.0481 mL | 0.2404 mL | 0.4808 mL | 1.2021 mL | |
| 30 mM | 0.0401 mL | 0.2003 mL | 0.4007 mL | 1.0017 mL | |
| 40 mM | 0.0301 mL | 0.1503 mL | 0.3005 mL | 0.7513 mL | |
| 50 mM | 0.0240 mL | 0.1202 mL | 0.2404 mL | 0.6010 mL | |
| 60 mM | 0.0200 mL | 0.1002 mL | 0.2003 mL | 0.5009 mL |
Larotaxel Related Classifications
HY-125374 Related Classifications
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Keywords
- Larotaxel
- 156294-36-9
- XRP9881
- XRP 9881
- XRP-9881
- Microtubule/Tubulin
- intracranial glioblastoma models
- P-glycoprotein-expressing multidrug-resistant cancer cells
- taxane-resistant tumor models
- cell cycle arrest
- blood-brain barrier penetration
- microtubule-stabilizing taxane
- cold-induced depolymerization
- mitotic spindle function
- microtubules
- oral activity
- Inhibitor
- inhibitor
- inhibit