CCT251236

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CCT251236

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1693731-40-6

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 anIC₅₀of 19 nM for inhibition of HSF1-mediatedHSP72induction.

IC₅₀& Target^[1]

HSP72

19 nM (IC₅₀, SK-OV-3 cells)

体外研究
(In Vitro)

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^[1].
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^[1].
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^[1].

Western Blot Analysis^[1]

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^[1]

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^[2].
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^[2].

Animal Model:	Athymic mice with SK-OV-3 cells^[2]
Dosage:	20 mg/kg; 33 days
Administration:	Oral adminstation
Result:	Was efficacious in SK-OV-3 cell induced-tumor mice model.

分子量

552.62

性状

Solid

Formula

C₃₂H₃₂N₄O₅

CAS 号

1693731-40-6

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 : ≥ 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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

*以上所有助溶剂都可在本网站选购。