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LXS196 Sale

(Synonyms: LXS196; IDE196) 目录号 : GC32811

A PKC inhibitor

LXS196 Chemical Structure

Cas No.:1874276-76-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,450.00
现货
2mg
¥720.00
现货
5mg
¥1,395.00
现货
10mg
¥2,115.00
现货
50mg
¥5,490.00
现货
100mg
¥8,280.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

LXS-196 is a PKC inhibitor (IC50s = 1.9 and 0.4 nM for PKCα and PKCθ, respectively).1 It is selective for PKCα and PKCθ over GSK3β (IC50 = 3,100 nM). It inhibits proliferation of TMD8 B cell lymphoma and 92.1 uveal melanoma cells (IC50s = 900 and 184 nM, respectively) but not SK-MEL-28 skin melanoma cells (IC50 = >10,000 nM).

1.Luzzio, M.J., Papillon, J., and Visser, M.S.Protein kinase C inhibitors and methods of their use(2016)

Chemical Properties

Cas No. 1874276-76-2 SDF
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
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1 mg 5 mg 10 mg
1 mM 2.1165 mL 10.5827 mL 21.1654 mL
5 mM 0.4233 mL 2.1165 mL 4.2331 mL
10 mM 0.2117 mL 1.0583 mL 2.1165 mL
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Research Update

A phase I trial of LXS196, a protein kinase C (PKC) inhibitor, for metastatic uveal melanoma

Br J Cancer 2023 Apr;128(6):1040-1051.PMID:36624219DOI:10.1038/s41416-022-02133-6.

Background: Up to 50% of patients with uveal melanoma develop metastases (MUM) with a poor prognosis and median overall survival of approximately 1 year. Methods: This phase I study evaluated the safety, tolerability, pharmacokinetics, pharmacodynamics and efficacy of the oral protein kinase C inhibitor LXS196 in 68 patients with MUM (NCT02601378). Patients received LXS196 doses ranging from 100-1000 mg once daily (QD; n = 38) and 200-400 mg twice daily (BID; n = 30). Results: First cycle dose-limiting toxicities (DLTs) were observed in 7/38 (18.4%) QD and 2/17 (11.8%) BID patients. Hypotension was the most common DLT, occurring at doses ≥500 mg/day, and manageable with LXS196 interruption and dose reduction. Median duration of exposure to LXS196 was 3.71 months (range: 1.81-15.28) for QD and 4.6 months (range: 0.33-58.32) for BID dosing. Clinical activity was observed in 6/66 (9.1%) evaluable patients achieving response (CR/PR), with a median duration of response of 10.15 months (range: 2.99-41.95); 45/66 had stable disease (SD) per RECIST v1.1. At 300 mg BID, the recommended dose for expansion, 2/18 (11.1%) evaluable patients achieved PR and 12/18 (66.7%) had SD. Conclusion: These results suggest manageable toxicity and encouraging clinical activity of single-agent LXS196 in patients with MUM.