Larotaxel
Based on 1 Customer Validation
Larotaxel (XRP9881) is a taxane analogue with preclinical activity against taxane-resistant breast cancer. Larotaxel (XRP9881) exerts its cytotoxic effect by promoting tubulin assembly and stabilizing microtubules, ultimately leading to cell death by apoptosis. It presents the ability to cross the blood brain barrier and has a much lower affinity for P-glycoprotein 1 than Docetaxel.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.50%
- CAS. Nr.: 156294-36-9
- Formel: C45H53NO14
- Molecular Weight:831.90
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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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] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 156294-36-9
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Appearance Solid
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Molecular Weight 831.90
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Reinheit & Dokumentation
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Data Sheet (280 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)
Verweise
[1]. Diéras V, et al. Phase II multicenter study of larotaxel (XRP9881), a novel taxoid, in patients with metastatic breast cancer who previously received taxane-based therapy. Ann Oncol. 2008 Jul;19(7):1255-60. [Content Brief]
[2]. Morris PG, et al. Novel anti-tubulin cytotoxic agents for breast cancer. Expert Rev Anticancer Ther. 2009 Feb;9(2):175-85. [Content Brief]
[3]. Zatloukal P, et al. Randomized multicenter phase II study of larotaxel (XRP9881) in combination with cisplatin or gemcitabine as first-line chemotherapy in nonirradiable stage IIIB or stage IV non-small cell lung cancer. J Thorac Oncol. 2008 Aug;3(8):894-901. [Content Brief]
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 |
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| 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
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