索尼吉布Sonidegib(NVP-LDE225 Erismodegib) Smo拮抗剂|CAS 956697-53-3（53275ES）

Sonidegib (NVP-LDE225, Erismodegib, NVPLDE225)，又称索尼吉布，是Smoothened (Smo)有效选择性拮抗剂，IC₅₀分别为1.3 nM (小鼠)和2.5 nM(人)，抑制Hedgehog (Hh)信号通路，临床上用于治疗基底细胞癌。Hh信号通路在胚胎发育、组织分化过程中起调控作用，Smo是Hh信号通路的激活子，Smo的异常激活与一些肿瘤的发生密切相关。

参考文献

1. Pan S, et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med Chem Lett. 2010 Mar 16;1(3):130-4.
2. Irvine DA, et al. Deregulated hedgehog pathway signaling is inhibited by the smoothened antagonist LDE225 (Sonidegib) in chronic phase chronic myeloid leukaemia. Sci Rep. 2016 May 9;6:25476.
3. Fendrich V, et al. Hedgehog inhibition with the orally bioavailable Smo antagonist LDE225 represses tumor growth and prolongs survival in a transgenic mouse model of islet cell neoplasms. Ann Surg. 2011 Nov;254(5):818-23; discussion 823.

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