LP-261
- CAS No.
- 915412-67-8
- Chemical Name:
- LP-261
- Synonyms
- LP-261;LP-261, 10 mM in DMSO;N-[3-(1H-indol-4-yl)-5-(2-methoxypyridine-4-carbonyl)phenyl]methanesulfonamide;Methanesulfonamide, N-[3-(1H-indol-4-yl)-5-[(2-methoxy-4-pyridinyl)carbonyl]phenyl]-;NCI-H522,tubulin polymerization,tumor,SW-620,BXPC-3,H522,anti-mitotic,inhibit,LP261,MCF-7,Inhibitor,Microtubule/Tubulin,LP 261,cancer,Jurkat,LP-261
- CBNumber:
- CB12628043
- Molecular Formula:
- C22H19N3O4S
- Molecular Weight:
- 421.47
- MDL Number:
- MFCD18782727
- MOL File:
- 915412-67-8.mol
| Boiling point | 700.6±70.0 °C(Predicted) |
|---|---|
| Density | 1.391±0.06 g/cm3(Predicted) |
| pka | 6.72±0.10(Predicted) |
| form | Solid |
| color | White to off-white |
| FDA UNII | O547O19Z01 |
LP-261 Chemical Properties,Uses,Production
Uses
LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM[1]. LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research[1].
in vivo
LP-261 (oral gavage; 4 mg/kg; single dose) displays rapid adsorption by the oral route (Tmax=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 (Vss) is 1.25 L/kg[1].LP-261 (oral gavage; 15 or 50 mg/kg; twice daily; 28 days) at 50mg/kg results in an approximately tumor volume of 130 mm3 versus 3769 mm3 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[1].
| Animal Model: | Human tumor xenograft model (Injected with NCI-H522 human non-small-cell) in NCr-nu mice[1] |
| 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. |
References
[1] Rupa S Shetty, et al. Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. J Med Chem. 2011 Jan 13;54(1):179-200 DOI:10.1021/jm100659v
LP-261 Preparation Products And Raw materials
Raw materials
Preparation Products
LP-261 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 32296 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38671 | 58 | |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd. | 17702719238 17702719238 | sales@sun-shinechem.com | China | 1039 | 64 |
| NCE Biomedical Co.,Ltd. | 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 | China | 1493 | 55 | |
| SPIRO PHARMA | eric_feng1954@126.com | China | 9248 | 55 | |
| Wuhan Sun-shine Bio-technology Corporation Limited | +86-027-6552-2453 | sales@sun-shinechem.com | China | 727 | 58 |
| InvivoChem | 13549236410 | sales@invivochem.cn | China | 6753 | 58 |
| Beijing Biocreative Technology Co., Ltd. | 15522676233 | 3007606172@qq.com | China | 1248 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24957 | 58 |
