| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
tubulin polymerization (EC50 = 3.2 μM)
LP-261 targets tubulin, binding at the colchicine binding site. By binding to tubulin, it inhibits tubulin polymerization. This leads to cell cycle arrest at the G2/M phase. The compound's activity is mediated through disruption of the mitotic spindle and microtubule dynamics. |
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| ln Vitro |
LP-261 shows a range of activity from 0.01μM to 0.38μM across the tested cell lines, and demonstrates potent G2/M block activity in multiple of them. The IC50 values for MCF-7, H522, Jurkat, SW-620, BXPC-3, and PC-3 are 0.01μM, 0.01μM, 0.02μM, 0.05μM, 0.05μM, and 0.07μM, respectively[1].
LP-261 demonstrates low micromolar potency; its EC50 value is 5.0 μM in the tubulin polymerization assay[1]. In a [3H]colchicine competition binding assay, LP-261 can rival colchicine for binding to tubulin. Its EC50 (3.2 μM) indicates that it can inhibit binding with a potency comparable to that of colchicine, and it can exhibit a 79% inhibition at a concentration of 30 μM[1]. LP-261 inhibits in vitro tubulin polymerization with an EC50 of 3.2 μM. It prevents microvessel outgrowth in the rat aortic ring assay and HUVEC cell proliferation at nanomolar concentrations. It shows a range of activity from 0.01 μM to 0.38 μM across tested cell lines. |
| ln Vivo |
LP-261 (oral gavage; 4 mg/kg; single dose) exhibits a moderate rate of elimination in rats, with a terminal half-life of 1.4 hours (0.2 hours) indicating rapid oral adsorption (Tmax=2.0 h), and a volume of distribution (Vss) of 1.25 L/kg[1].
LP-261 (oral gavage; 15 or 50 mg/kg; twice daily; 28 days) at 50 mg/kg causes an approximate tumor volume of 130 mm3, which is 96% less than the mean tumor volume in the vehicle treated group, which was 3769 mm3. In this mouse model, LP-261 at 15 mg/kg results in a 41% inhibition after 28 days[1].
LP-261 inhibits the growth of human non-small cell lung cancer (NCI-H522) in vivo. It is a potent and orally active anti-mitotic agent. It has shown broad-spectrum antitumor activity in preclinical models. The compound has favorable pharmacokinetic properties supporting oral dosing. |
| Enzyme Assay |
Non-cell-based tubulin polymerization assays for LP-261 use purified tubulin protein. The compound is incubated with tubulin and GTP at varying concentrations. Tubulin polymerization is measured by turbidity (absorbance at 340 nm) over time. The EC50 for inhibition of polymerization is determined. Colchicine binding site competition assays may be performed using radiolabeled colchicine.
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| Cell Assay |
Cellular assays for LP-261 utilize cancer cell lines such as HUVEC (endothelial cells) and NCI-H522 (lung cancer). Cells are treated with the compound at various concentrations. Cell proliferation is measured using standard viability assays (e.g., MTT, CellTiter-Glo). Cell cycle analysis by flow cytometry is performed to confirm G2/M arrest. Angiogenesis inhibition is assessed in endothelial cell tube formation assays.
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| Animal Protocol |
Human tumor xenograft model (Injected with NCI-H522 human non-small-cell) in NCr-nu mice[1]
15 or 50 mg/kg Oral gavage; 15 or 50 mg/kg; twice daily; 28 days In vivo animal models for LP-261 include xenograft studies in immunodeficient mice bearing human tumor cell lines such as NCI-H522. The compound is administered orally at various doses. Tumor growth inhibition is monitored over time. Angiogenesis inhibition may be assessed in the rat aortic ring assay in vivo. Pharmacokinetic parameters are measured to support oral dosing. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of LP-261 include CAS number 915412-67-8. The compound is orally active and has favorable pharmacokinetic properties supporting oral dosing. Purity is >98%. Detailed PK parameters such as half-life and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
LP-261 is a tubulin-targeting anticancer agent. It has shown broad-spectrum antitumor activity and is a potent inhibitor of angiogenesis. Detailed toxicity data are not extensively reported. The compound is a research tool for studying microtubule function and anti-mitotic therapy. It holds therapeutic potential for diverse malignancies.
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| References | |
| Additional Infomation |
LP-261 is a novel tubulin targeting anticancer agent. It has CAS number 915412-67-8. The compound binds at the colchicine site on tubulin and induces G2/M arrest. It is a potent and orally active anti-mitotic agent. It inhibits tubulin polymerization with an EC50 of 3.2 μM and inhibits HUVEC proliferation at nanomolar concentrations.
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| Molecular Formula |
C22H19N3O4S
|
|---|---|
| Molecular Weight |
421.47
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| Exact Mass |
421.11
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| Elemental Analysis |
C, 62.69; H, 4.54; N, 9.97; O, 15.18; S, 7.61
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| CAS # |
915412-67-8
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| Related CAS # |
915412-67-8
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| PubChem CID |
15603282
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| Appearance |
White to off-white solid powder
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| LogP |
4.994
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
710
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=NC=CC(=C1)C(=O)C2=CC(=CC(=C2)C3=C4C=CNC4=CC=C3)NS(=O)(=O)C
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| InChi Key |
YUVDELGTFILMBB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H19N3O4S/c1-29-21-13-14(6-8-24-21)22(26)16-10-15(11-17(12-16)25-30(2,27)28)18-4-3-5-20-19(18)7-9-23-20/h3-13,23,25H,1-2H3
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| Chemical Name |
N-[3-(1H-indol-4-yl)-5-(2-methoxypyridine-4-carbonyl)phenyl]methanesulfonamide
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| Synonyms |
LP261; LP-261; LP 261
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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: ~33.3 mg/mL (~79.1 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3726 mL | 11.8632 mL | 23.7265 mL | |
| 5 mM | 0.4745 mL | 2.3726 mL | 4.7453 mL | |
| 10 mM | 0.2373 mL | 1.1863 mL | 2.3726 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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