LDE225 Diphosphate|1218778-77-8|(Erismodegib diphosphate; LDE225 diphosphate; NVP-LDE225 diphosphate)-陌孚医药/Medlife

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LDE225 Diphosphate (Synonyms: Erismodegib diphosphate; LDE225 diphosphate; NVP-LDE225 diphosphate)

目录号: PC15834 纯度: ≥98%

CAS No. :1218778-77-8

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PC15834-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥735.00	请登录

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中文名称	LDE225 Diphosphate
英文名称	LDE225 Diphosphate
英文别名	N-[6-[(2S,6R)-2,6-dimethylmorpholin-4-yl]pyridin-3-yl]-2-methyl-3-[4-(trifluoromethoxy)phenyl]benzamide,phosphoric acid;UNII-W421AI34UW;Erismodegib Diphosphate;LDE225 Diphosphate;Sonidegib phosphate;NVP-LDE 225 Diphosphate;CS-1175;;LDE 225 phosphate;rel-N-[6-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-3-pyridinyl]-2-methyl-4'-(trifluoromethoxy)-[1,1'-biphenyl]-3-carboxamide phosphate (1:2);LDE225 (Diphosphate);Sonidegib phosphate;LDE225 Diphosphate;sonidegib diphosphate;Sonidegib (diphosphate);W421AI34UW;Sonidegib phosphate [USAN:INN];Odomzo (TN);sonidegib bisphosphate;Sonidegib phosphate (USAN);AOB87343;BCP11860;3888AH;C26H26F3N3O3.2H3O4P;SB16677;(1,1'-Biphenyl)-3-carboxamide, N-(6-((2R,6S)-
Cas No.	1218778-77-8
分子式	C₂₆H₃₂F₃N₃O₁₁P₂
分子量	681.49
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Sonidegib diphosphate (Erismodegib 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.

性状

Solid

IC50 & Target[1][2]

IC50: 1.3 nM (mSmo), 2.5 nM (hSmo)

体外研究(In Vitro)

The IC₅₀ values for Sonidegib (NVP-LDE225) for the major human CYP450 drug metabolizing enzymes is greater than 10 μM. Sonidegib (LDE225), a small molecule, clinically investigated SMO inhibitor, used alone and in combination with Nilotinib, inhibits the Hh pathway in CD34 chronic phase (CP)-chronic myeloid leukaemia (CML) cells, reducing the number and self-renewal capacity of CML leukaemia stem cell (LSC). Sonidegib interacts directly with SMO, in a similar fashion to cyclopamine, to reduce expression of downstream Hh signaling targets. Primary CD34 CP-CML cells are cultured in serum free media (SFM)±Sonidegib for 6, 24 and 72 hours (h). At 72 h, while there is variability between the biological samples, GLI1 is significantly downregulated following exposure to Sonidegib (10 nM; 0.78-fold and 100 nM; 0.73-fold, respectively (p<0.01).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Sonidegib (NVP-LDE225) is a weak base with a measured pK_a of 4.2 and exhibits relatively poor aqueous solubility. In the subcutaneous Ptchp53 medulloblastoma allograft mouse model, Sonidegib demonstrates dose-related antitumor activity after 10 days of oral administration of a suspension of the diphosphate salt. At a dose of 5 mg/kg/day qd, Sonidegib significantly inhibits tumor growth, corresponding to a T/C value of 33% (p<0.05 as compared to vehicle controls). When dosed at 10 and 20 mg/kg/day qd, Sonidegib affords 51 and 83% regression, respectively. Bone marrow cells and spleen cells from a subset of treated mice are transplanted into secondary recipient mice. Transplantation of either bone marrow (BM) or spleen cells from mice treated with Sonidegib (LDE225)+Nilotinib results in reduced white cell count (WCC) and reduces leukaemia development in secondary recipients compared to Sonidegib or Nilotinib alone.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (146.74 mM; Need ultrasonic)

H₂O : 0.25 mg/mL (0.37 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4674 mL	7.3369 mL	14.6737 mL
5 mM	0.2935 mL	1.4674 mL	2.9347 mL
10 mM	0.1467 mL	0.7337 mL	1.4674 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.67 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.67 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.67 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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