CCT251236|cas:1693731-40-6|西域试剂

CCT251236,98.0%

产品编号：Bellancom-101026| CAS NO：1693731-40-6| 分子式：C₃₂H₃₂N₄O₅| 分子量：552.62

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货号	价格	库存与货期
Bellancom-101026	￥1100.00	杭州北京（现货）
Bellancom-101026	￥3300.00	杭州北京（现货）
Bellancom-101026	￥5000.00	杭州北京（现货）
Bellancom-101026	￥15000.00	杭州北京（现货）
Bellancom-101026	￥21000.00	杭州北京（现货）

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CCT251236

产品介绍

CCT251236 是通过热休克转录因子 1 (hsf1) 表型筛选得到的有口服活性的吡啶配体，抑制 HSF1 介导的 HSP72 诱导的 IC₅₀ 值为 19 nM。

生物活性

CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC₅₀ of 19 nM for inhibition of HSF1-mediated HSP72 induction.

体外研究

CCT251236 (0-100 nM; 24hours) displays a desired balance of in vitro properties, while maintaining excellent cellular activity with a pIC50=7.73 ± 0.07 (IC₅₀=19 nM) for inhibition of HSF1-mediated HSP72 induction. The free GI₅₀ is 1.1 nM in SK-OV-3 cells that calculated from the free fraction in the cell assay.
CCT251236 (0-100 nM; 24 hours) blocks 17-AAG induced he HSF1-mediated heat-shock proteins, HSP72 and HSP27 expression as a concentration manner in SK-OV-3 cells.
CCT251236 (0-100 nM; 24 hours), pre-treated with 250 nM 17-AAG for 6h, blocks the induction of HSPA1A mRNA by 17-AAG in a dosedependent manner.

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

Western Blot Analysis

Cell Line:	SK-OV-3 cells
Concentration:	0 nM; 10 nM; 100 nM
Incubation Time:	24 hours
Result:	Inhibited HSP72 and HSP27 expression at the dose of 10 nM.

RT-PCR

Cell Line:	SK-OV-3 cells
Concentration:	0 nM; 10 nM; 100 nM and 1000 nM
Incubation Time:	24 hours
Result:	Decreased HSPA1A mRNA level.

体内研究
(In Vivo)

CCT251236 (oral adminstation; 5 or 20 mg/kg) in nontumor bearing immunocompetent BALB/c mice exhibits free C_av^0-24h value of 2.0 nM and 1.2 nM, respectively.
CCT251236 (oral adminstation; 20 mg/kg; 33 days) has a clear therapeutic efficacy in mice with a tumor growth inhibition (%TGI) of 70% based on final tumor volumes. After 33 days, the mean tumor weights decreases 64% when compares to control group. In addition, the compound’s basicity and high volume of distribution shows in tumor withtumor concentrations of CCT251236 as high as 940 nM.

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

Animal Model:	Athymic mice with SK-OV-3 cells
Dosage:	20 mg/kg; 33 days
Administration:	Oral adminstation
Result:	Was efficacious in SK-OV-3 cell induced-tumor mice model.

体内研究

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

Animal Model:	Athymic mice with SK-OV-3 cells
Dosage:	20 mg/kg; 33 days
Administration:	Oral adminstation
Result:	Was efficacious in SK-OV-3 cell induced-tumor mice model.

体内研究

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

Animal Model:	Athymic mice with SK-OV-3 cells
Dosage:	20 mg/kg; 33 days
Administration:	Oral adminstation
Result:	Was efficacious in SK-OV-3 cell induced-tumor mice model.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 150 mg/mL (271.43 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	1.8096 mL	9.0478 mL	18.0956 mL
5 mM	0.3619 mL	1.8096 mL	3.6191 mL
10 mM	0.1810 mL	0.9048 mL	1.8096 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 (4.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.52 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 ddH₂O 中，得到澄清透明的生理盐水溶液