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Sonidegib diphosphate {[allProObj[0].p_purity_real_show]}

货号:A624949 同义名: NVP-LDE225 diphosphate; Erismodegib diphosphate

Sonidegib diphosphate是一种强效且选择性的 Smo 抑制剂,在小鼠和人类 Smo 的结合实验中的 IC50 分别为 1.3 nM 和 2.5 nM。

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Sonidegib diphosphate 化学结构 CAS号:1218778-77-8
Sonidegib diphosphate 化学结构
CAS号:1218778-77-8
Sonidegib diphosphate 3D分子结构
CAS号:1218778-77-8
Sonidegib diphosphate 化学结构 CAS号:1218778-77-8
Sonidegib diphosphate 3D分子结构 CAS号:1218778-77-8
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Sonidegib diphosphate 纯度/质量文件 产品仅供科研

货号:A624949 标准纯度: {[allProObj[0].p_purity_real_show]}
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Sonidegib diphosphate 生物活性

描述 LDE225 diphosphate is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.

Sonidegib diphosphate 细胞实验

Cell Line
Concentration Treated Time Description References
BV2 microglial cells 10 µM 24 hours Inhibited LPS-induced JNK phosphorylation Int J Mol Sci. 2022 Sep 13;23(18):10590
BV2 microglial cells 10 µM 24 hours Inhibited the LPS-induced IκBα phosphorylation and NF-κB nuclear translocation Int J Mol Sci. 2022 Sep 13;23(18):10590
BV2 microglial cells 10 µM 24 hours Inhibited the LPS-induced expression of iNOS and COX-2 Int J Mol Sci. 2022 Sep 13;23(18):10590
BV2 microglial cells 10 µM 24 hours Suppressed LPS-stimulated cell migration Int J Mol Sci. 2022 Sep 13;23(18):10590
BV2 microglial cells 10 µM 24 hours Inhibited LPS-induced MKK4 phosphorylation Int J Mol Sci. 2022 Sep 13;23(18):10590
BV2 microglial cells 10 µM 24 hours Inhibited LPS-induced c-Jun phosphorylation Int J Mol Sci. 2022 Sep 13;23(18):10590
BV2 microglial cells 30 µM 24 hours Reduced the LPS-induced production of IL-1β, IL-6, TNF-α, and NO Int J Mol Sci. 2022 Sep 13;23(18):10590
HS-5 cells 10 µM 48 hours To investigate the effect of Sonidegib on the adhesion of HS-5 bone marrow stromal spheroids to OCI-AML3 cells. Results showed that Sonidegib significantly prolonged the contact time required for leukemia cells to establish adhesive connections with the bone marrow stromal spheroid. Biomedicines. 2025 Feb 25;13(3):578
OCI-AML3 cells 10 µM 48 hours To investigate the effect of Sonidegib on the adhesion of OCI-AML3 cells to HS-5 bone marrow stromal spheroids. Results showed that Sonidegib significantly increased the minimum cell-to-cell adhesion time required for leukemic cells to establish adhesive bonds with bone marrow stromal cells, indicating a reduction in their adhesive properties. Biomedicines. 2025 Feb 25;13(3):578

Sonidegib diphosphate 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Human Patients with locally advanced basal cell carcinoma Oral 200 mg/day Once daily for a median duration of 7.8 months (range 6-11 months) To evaluate the efficacy and safety of Sonidegib alone or in combination with surgical excision for the treatment of locally advanced basal cell carcinomas. Results showed that 15 out of 29 lesions treated with Sonidegib alone achieved complete remission (CR), and 14 had partial remission (PR). All lesions treated with Sonidegib in association with surgical excision achieved CR. Oncologist. 2022 Jun 8;27(6):e533
ICR mice LPS-induced neuroinflammation model Oral 40 mg/kg Once daily for 7 days Attenuated IL-6 and TNF-α levels in the brains of LPS-treated mice Int J Mol Sci. 2022 Sep 13;23(18):10590
BALB/c mice Breast cancer bone metastasis model Oral 50 mg/kg Once daily until the mice were sacrificed To evaluate the inhibitory effect of Sonidegib on breast cancer bone metastasis. Sonidegib treatment reduced ALP expression around tumor cells and recovered NK cell infiltration in bone lesions, leading to alleviated bone metastasis burden, and extended survival of the mice. Cell Res. 2023 Jun;33(6):464-478

Sonidegib diphosphate 参考文献

[1]Irvine DA, Zhang B, 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.

[2]Pan S, Wu X, et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med Chem Lett. 2010 Mar 16;1(3):130-4.

Sonidegib diphosphate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.47mL

0.29mL

0.15mL

7.34mL

1.47mL

0.73mL

14.67mL

2.93mL

1.47mL

Sonidegib diphosphate 技术信息

CAS号1218778-77-8
分子式C26H32F3N3O11P2
分子量 681.49
SMILES Code O=C(C1=C(C)C(C(C=C2)=CC=C2OC(F)(F)F)=CC=C1)NC3=CC=C(N=C3)N4C[C@@H](C)O[C@@H](C)C4.O=P(O)(O)O.O=P(O)(O)O
MDL No. MFCD16627994
别名 NVP-LDE225 diphosphate; Erismodegib diphosphate; Sonidegib; NVP-LDE225; Erismodegib; LDE225 (phosphate); LDE225 diphosphate
运输蓝冰
InChI Key RWIVSVMMGFFZIJ-VWDRLOGHSA-N
Pubchem ID 45138699
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

DMSO: 105 mg/mL(154.07 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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