| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| 100mg |
Purity: ≥98%
| Targets |
Larotaxel targets the β-tubulin subunit of microtubules, binding to the taxane-binding site and stabilizing microtubule polymers. This stabilization prevents microtubule depolymerization, leading to mitotic arrest at the G₂/M phase of the cell cycle and subsequent apoptosis. Unlike paclitaxel, larotaxel is not a substrate for P-glycoprotein, making it effective against multidrug-resistant tumors that overexpress this efflux pump. It also demonstrates improved brain penetration.
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| ln Vitro |
In vitro, larotaxel demonstrates potent antiproliferative activity against a wide range of cancer cell lines, including those resistant to paclitaxel and docetaxel due to P-glycoprotein overexpression or tubulin mutations. IC₅₀ values are typically in the low nanomolar range. It induces G₂/M cell cycle arrest and apoptosis in a dose-dependent manner. Larotaxel also shows activity in cell lines with brain metastases.
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| ln Vivo |
In vivo, larotaxel has demonstrated significant antitumor activity in various xenograft models, including tumors resistant to paclitaxel and docetaxel. It has shown activity in models of breast cancer, lung cancer, prostate cancer, and pancreatic cancer. Larotaxel has also demonstrated the ability to penetrate the blood-brain barrier and exhibit activity against brain metastases. Oral administration has been shown to be effective in some models.
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| Enzyme Assay |
Antiproliferative assays: Cancer cell lines are cultured in appropriate media and treated with larotaxel at various concentrations (typically 0.1-100 nM) for 48-72 hours. Cell viability is assessed using MTT, SRB, or CellTiter-Glo assays. IC₅₀ values are calculated from dose-response curves. For mechanism studies, cell cycle analysis is performed by flow cytometry and apoptosis is evaluated by Annexin V/PI staining and caspase activity assays.
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| Cell Assay |
Cancer cell lines including paclitaxel-sensitive and -resistant lines are cultured in RPMI-1640 or DMEM with 10% FBS at 37°C with 5% CO₂. Cells are seeded in 96-well plates and treated with larotaxel at various concentrations for 48-72 hours. Cell viability is assessed and IC₅₀ values are calculated. For tubulin polymerization assays, purified tubulin is incubated with larotaxel and polymerization is monitored spectrophotometrically.
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| Animal Protocol |
In vivo efficacy studies are conducted in tumor xenograft models. Larotaxel is administered intravenously, orally, or via other routes at specified doses. Tumor growth is monitored over time. Pharmacokinetic parameters are assessed by measuring compound concentrations in plasma and tissues (including brain). Efficacy against brain metastases is evaluated in appropriate models. Toxicity and tolerability are monitored.
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| ADME/Pharmacokinetics |
Larotaxel has molecular formula C₄₅H₅₃NO₁₄ and molecular weight approximately 831.9. It is a semisynthetic taxane derivative with improved properties over first-generation taxanes. The compound is typically stored as a powder at -20°C and is soluble in DMSO and other organic solvents. Detailed physicochemical properties, formulation guidelines, and handling conditions are available from chemical suppliers.
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| References |
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| Additional Infomation |
Larotaxel has been used in clinical trials for the treatment of various cancers, including metastatic cancer, breast cancer, breast tumors, and pancreatic tumors. Larotaxel is a semi-synthetic derivative of the taxane compound 10-deacetylated baccatin III and possesses potential antitumor activity. Larotaxel binds to tubulin, promoting microtubule assembly and stabilization, and preventing microtubule depolymerization, thereby inhibiting cell proliferation. Because it is not readily targeted by P-glycoprotein-associated resistance mechanisms, this drug may be effective in treating multidrug-resistant tumors. Larotaxel can cross the blood-brain barrier.
Larotaxel (XRP-9881) is a semisynthetic taxane derivative developed as a next-generation anticancer agent. It exhibits potent antimicrotubule activity and is effective against taxane-resistant tumors, including those that overexpress P-glycoprotein. Larotaxel also demonstrates improved penetration of the blood-brain barrier and oral bioavailability. The compound has been investigated in clinical trials for various solid tumors including breast, lung, prostate, and pancreatic cancers. |
| Molecular Formula |
C45H53NO14
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|---|---|
| Molecular Weight |
831.900634527206
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| Exact Mass |
831.346
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| CAS # |
156294-36-9
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| PubChem CID |
6918260
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
889.3±65.0 °C at 760 mmHg
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| Flash Point |
491.7±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.613
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| LogP |
7.06
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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 |
1790
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| Defined Atom Stereocenter Count |
11
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| SMILES |
CC1=C2C(C(=O)C34CC3CC5C(C4C(C(C2(C)C)(CC1OC(=O)C(C(C6=CC=CC=C6)NC(=O)OC(C)(C)C)O)O)OC(=O)C7=CC=CC=C7)(CO5)OC(=O)C)OC(=O)C
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| InChi Key |
DXOJIXGRFSHVKA-BZVZGCBYSA-N
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| InChi Code |
InChI=1S/C45H53NO14/c1-23-29(57-39(52)33(49)32(26-15-11-9-12-16-26)46-40(53)60-41(4,5)6)21-45(54)37(58-38(51)27-17-13-10-14-18-27)35-43(36(50)34(56-24(2)47)31(23)42(45,7)8)20-28(43)19-30-44(35,22-55-30)59-25(3)48/h9-18,28-30,32-35,37,49,54H,19-22H2,1-8H3,(H,46,53)/t28-,29+,30-,32+,33-,34-,35+,37+,43-,44+,45-/m1/s1
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| Chemical Name |
(1S,2S,4S,7R,8aR,9aS,10aR,12aS,12bR)-1-(benzoyloxy)-4-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-2-hydroxy-5,13,13-trimethyl-8-oxo-1,3,4,7,8,9,9a,10,10a,12b-decahydro-2H-2,6-methanocyclodeca[3,4]cyclopropa[4,5]benzo[1,2-b]oxete-7,12a(12H)-diyl
diacetate
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| Synonyms |
XRP9881 XRP 9881 XRP-9881 RPR109881 RPR-109881 RPR
109881 RPR109881A RPR 109881 RPR-109881A PNU100940 PNU-100940 PNU
100940.
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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) |
DMSO : ≥ 50 mg/mL (~60.10 mM)
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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 | 1.2021 mL | 6.0103 mL | 12.0207 mL | |
| 5 mM | 0.2404 mL | 1.2021 mL | 2.4041 mL | |
| 10 mM | 0.1202 mL | 0.6010 mL | 1.2021 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.
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