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Darovasertib

CAS No. : 1874276⁻⁷6-2

MCE 国际站：Darovasertib

产品活性：Darovasertib (LXS196) 是有效的、选择性的和具有口服活性的蛋白激酶C (PKC) 抑制剂，对 PKCα、PKCθ 和 GSK3β 的 IC₅₀ 值分别为 1.9 nM、0.4 nM 和 3.1 μM。Darovasertib 有潜力用于葡萄膜黑素瘤的研究。

研究领域：Epigenetics | TGF-beta/Smad

作用靶点：PKC

In Vitro: 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.

In Vivo: Darovasertib (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.

相关产品：Clinical Compound Library Plus | Bioactive Compound Library Plus | Epigenetics Compound Library | Kinase Inhibitor Library | TGF-beta/Smad Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Cytoskeleton Compound Library | Orally Active Compound Library | Phorbol 12-myristate 13-acetate | Staurosporine | Ionomycin | Go 6983 | Midostaurin | Bisindolylmaleimide I | Mitoxantrone | Fasudil Hydrochloride | Sotrastaurin | Rottlerin | Enzastaurin | Afuresertib | Chelerythrine chloride | Ingenol Mebutate | K-252a | Ro 31-8220 mesylate | Phorbol 12,13-dibutyrate | D-erythro-Sphingosine | CGP60474 | Verbascoside | (-)-Indolactam V | Ruboxistaurin hydrochloride | CMPD101 | TPPB | Go6976 | Daphnetin | DCP-LA

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