| Identification | Back Directory | [Name]
LP-261 | [CAS]
915412-67-8 | [Synonyms]
LP-261
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 | [Molecular Formula]
C22H19N3O4S | [MDL Number]
MFCD18782727 | [MOL File]
915412-67-8.mol | [Molecular Weight]
421.47 |
| Chemical Properties | Back Directory | [Boiling point ]
700.6±70.0 °C(Predicted) | [density ]
1.391±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
6.72±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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 |
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| Company Name: |
NCE Biomedical Co.,Ltd.
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| Tel: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
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www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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