Crenigacestat (Synonyms:LY3039478)
目录号 : KM3004 CAS No. : 1421438-81-4 纯度 : 98%

Crenigacestat (LY3039478) 是具有口服活性的 Notch 和 γ-secretase 的抑制剂,其在多种肿瘤细胞中的 IC50 为 ∼1nM。

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2mg
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5mg
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10mg
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25mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested.

体外研究

Crenigacestat (100 nM) exhibits anti-cancer activity in K07074 cells (a primary mouse liver tumor cell line).
Crenigacestat (LY3039478) decreases expression of Myc and cyclin A1 (part of the NOTCH-driven proliferative signature) in murine and human model systems. Crenigacestat (LY3039478) treatment also leads to G0/G1 cell cycle arrest in CCRCC cells.

Cell Viability Assay.

Cell Line: K07074 cells.
Concentration: 100 nM.
Incubation Time: 24-96 hours.
Result: Effectively reduced the growth of K07074 cells.
体内研究

Crenigacestat (8 mg/kg, oral gavage three times a week) resulted in significantly increases survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC.

Animal Model: CCRCC xenografts were established in NOD-scid IL2R null mice with subcutaneous implantation using the 769-P cell line.
Dosage: 8 mg/kg.
Administration: Oral gavage three times a week.
Result: Resulted in increased overall survival when compared with vehicle control in CCRCC xenografts.
分子式
C22H23F3N4O4
分子量
464.44
CAS号
1421438-81-4
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 34 mg/mL (73.21 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1531 mL 10.7657 mL 21.5313 mL
5 mM 0.4306 mL 2.1531 mL 4.3063 mL
10 mM 0.2153 mL 1.0766 mL 2.1531 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.38 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.38 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。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.38 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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科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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