≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC 50 of 3.2 μM LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research
In Vitro
LP-261 shows potent G2/M block activity in multiple cell lines and exhibits a range of activity from 0.01μM to 0.38 μM across the tested cell lines, the IC 50 values for MCF-7, H522, Jurkat, SW-620, BXPC-3, and PC-3 values are 0.01 μM, 0.01 μM, 0.02 μM, 0.05 μM, 0.05μM and 0.07 μM, respectively. LP-261 exhibits low micromolar potency in the tubulin polymerization assay, the EC 50 value of LP-261 is 5.0 μM. LP-261 has the ability to compete with colchicine for binding to tubulin in a [ 3 H]colchicine competition binding assay, the EC 50 (3.2 μM) for LP-261 to inhibit the binding with a potency similar to that of colchicine itself, and it exhibits a 79% inhibition at a conctration of 30 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
LP-261 (oral gavage; 4 mg/kg; single dose) displays rapid adsorption by the oral route (T max =2.0 h), the terminal half-life of 1.4 h ( 0.2 h indicated a moderate rate of elimination in rat, and the volume of distribution (V ss ) is 1.25 L/kg . LP-261 (oral gavage; 15 or 50 mg/kg; twice daily; 28 days) at 50mg/kg results in an approximately tumor volume of 130 mm 3 versus 3769 mm 3 in the vehicle treated group, this represents a 96% reduction in mean tumor volume. Meanwhile, LP-261 at 15 mg/kg leads to a 41% inhibition after 28 days in this mouse model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Human tumor xenograft model (Injected with NCI-H522 human non-small-cell) in NC r-nu mice Dosage: 15 or 50 mg/kg Administration: Oral gavage; 15 or 50 mg/kg; twice daily; 28 days Result: Had potent anti-tumor efficacy at high dosage and exhibited no significant changes in body weights.
Form:Solid
IC50& Target:EC50: 3.2 μM (tubulin polymerization)
| Canonical Smiles | COC1=NC=CC(=C1)C(=O)C2=CC(=CC(=C2)C3=C4C=CNC4=CC=C3)NS(=O)(=O)C |
|---|---|
| IUPAC Name | N-[3-(1H-indol-4-yl)-5-(2-methoxypyridine-4-carbonyl)phenyl]methanesulfonamide |
| InChIKey | YUVDELGTFILMBB-UHFFFAOYSA-N |
| 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 |
| Isomeric SMILES | COC1=NC=CC(=C1)C(=O)C2=CC(=CC(=C2)C3=C4C=CNC4=CC=C3)NS(=O)(=O)C |
| Alternate CAS | 915412-67-8 |
| PubChem CID | 15603282 |
| MeSH Entry Terms | LP 261;LP-261;LP261 cpd;N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide |
| Molecular Weight | 421.47 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organic oxygen compounds |
| Class | Organooxygen compounds |
| Subclass | Carbonyl compounds |
| Intermediate Tree Nodes | Ketones - Aryl ketones - Phenylketones |
| Direct Parent | Aryl-phenylketones |
| Alternative Parents | Sulfanilides Pyridinecarboxylic acids and derivatives Indoles Benzoyl derivatives Alkyl aryl ethers Organosulfonamides Organic sulfonamides Pyrroles Heteroaromatic compounds Aminosulfonyl compounds Azacyclic compounds Organonitrogen compounds Organic oxides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Aryl-phenylketone - Sulfanilide - Indole - Indole or derivatives - Pyridine carboxylic acid or derivatives - Benzoyl - Alkyl aryl ether - Monocyclic benzene moiety - Pyridine - Organic sulfonic acid amide - Organosulfonic acid amide - Benzenoid - Organic sulfonic acid or derivatives - Pyrrole - Heteroaromatic compound - Organosulfonic acid or derivatives - Sulfonyl - Aminosulfonyl compound - Organoheterocyclic compound - Azacycle - Ether - Organic nitrogen compound - Organosulfur compound - Organonitrogen compound - Hydrocarbon derivative - Organic oxide - Aromatic heteropolycyclic compound |
| Description | This compound belongs to the class of organic compounds known as aryl-phenylketones. These are aromatic compounds containing a ketone substituted by one aryl group, and a phenyl group. |
| External Descriptors | Not available |
| Solubility | DMSO : 33.33 mg/mL (79.08 mM; Need ultrasonic) |
|---|---|
| Molecular Weight | 421.500 g/mol |
| XLogP3 | 3.200 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 6 |
| Exact Mass | 421.11 Da |
| Monoisotopic Mass | 421.11 Da |
| Topological Polar Surface Area | 110.000 Ų |
| Heavy Atom Count | 30 |
| Formal Charge | 0 |
| Complexity | 710.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
