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LXS196
本半岛bd体育手机客户端 不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LXS196图片
CAS NO: 1874276-76-2
包装与价格:
包装 价格(元)
10mM (in 1mL DMSO) 电议
2mg 电议
5mg 电议
10mg 电议
50mg 电议
100mg 电议

半岛bd体育手机客户端 介绍
LXS196 (LXS196) 是一种有效的、选择性和口服活性的蛋白激酶 C (PKC) 抑制剂,IC50 值为 1.9 nM、0.4 nM 和 3.1和葛兰素史克3β,分别。 LXS196 具有用于葡萄膜黑色素瘤研究的潜力。
Cas No. 1874276-76-2
别名 LXS196; IDE196
Canonical SMILES NC1=C(C(NC2=C(N3CCC(C)(N)CC3)C=CC=N2)=O)N=C(C4=NC=CC=C4C(F)(F)F)C=N1
分子式 C22H23F3N8O
分子量 472.47
溶解度 DMSO : ≥ 100 mg/mL (211.65 mM)
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. It can be used for the treatment of uveal melanoma[1][2].

Upon oral administration, protein kinase C inhibitor LXS196 binds to and inhibits PKC, which prevents the activation of PKC-mediated signaling pathways. This may lead to the induction of cell cycle arrest and apoptosis in susceptible tumor cells. PKC, a serine/threonine protein kinase overexpressed in certain types of cancer cells, is involved in tumor cell differentiation, proliferation, invasion and survival[1].

LXS196 (compound 9) (15, 30, 75, 150 mg/kg, P.O., mice) shows improved efficacy (regression) in a 92.1 GNAQ uveal melanoma xenograft model in a dose-dependently manner[2].|| Animal Model:|Mice implanted with 92.1 GNAQ mutant uveal melanoma cells[2].|Dosage:|15, 30, 75, 150 mg/kg|Administration:|P.O. (bid) for 35 days|Result:|Dose-dependently suppressed the tumor growth.

[1]. Protein Kinase C Inhibitor LXS196 [2]. US20180179181.

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