LP-261

O547O19Z01 | MS-27398 | HY-14389 | LP-261 | SB19852 | N-[3-(1H-indol-4-yl)-5-(2-methoxypyridine-4-carbonyl)phenyl]methanesulfonamide | SCHEMBL3933505 | N-(3-(1h-indol-4-yl)-5-(2 methoxyisonicotinoyl)phenyl)methanesulfonamide | Q27285346 | UNII-O547O19Z01

LP-261

L647531-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

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)

LP-261 是一种有效的口服活性抗有丝分裂剂，对体外微管蛋白聚合有抑制作用，EC 50 为 3.2 μM。LP-261 可抑制人非小细胞肺肿瘤（NCI-H522）在体内的生长，可用于癌症研究。

915412-67-8

C22H19N3O4S

421.47 g/mol

15603282

COC1=NC=CC(=C1)C(=O)C2=CC(=CC(=C2)C3=C4C=CNC4=CC=C3)NS(=O)(=O)C

N-[3-(1H-indol-4-yl)-5-(2-methoxypyridine-4-carbonyl)phenyl]methanesulfonamide

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

YUVDELGTFILMBB-UHFFFAOYSA-N

COC1=NC=CC(=C1)C(=O)C2=CC(=CC(=C2)C3=C4C=CNC4=CC=C3)NS(=O)(=O)C

15603282

915412-67-8

LP 261;LP-261;LP261 cpd;N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide

DMSO : 33.33 mg/mL (79.08 mM; Need ultrasonic)

2

6

6

421.11 Da

421.11 Da

110.000 Ų

30

0

710.000

0

1

3.200