666-15|cas:1433286-70-4|西域试剂

666-15,99.74%

产品编号：Bellancom-101120| CAS NO：1433286-70-4| 分子式：C₃₃H₃₁Cl₂N₃O₅| 分子量：620.52

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-101120	￥1150.00	杭州北京（现货）
Bellancom-101120	￥1850.00	杭州北京（现货）
Bellancom-101120	￥3900.00	杭州北京（现货）
Bellancom-101120	￥6500.00	杭州北京（现货）
Bellancom-101120	￥10500.00	杭州北京（现货）

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666-15

产品介绍

666-15 是一种有效的选择性 CREB 抑制剂，IC₅₀ 为 81 nM。666-15 抑制乳腺癌异种移植模型中的肿瘤生长。

生物活性

666-15 is a potent and selective CREB inhibitor with an IC₅₀ of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.

体外研究

666-15 (73 nM; for 12 hours) significantly blocks the effects caused by MSN overexpression, including cell proliferation, invasion, soft agar colony formation ability, and the expression of CREB downstream genes. 666-15 inhibits MSN overexpression-induced CREB phosphorylation.
666-15 (1μM; pretreated 2 hour) effectively inhibits PE-induced CREB phosphorylation. 666-15 significantly decreases the protein expression of ANP and β-MHC and inhibits the activation of ER stress, including the expression of GRP78, CHOP, ATF6, and the phosphorylation of IRE1 in PE + siRNA + 666-15 group and PE + si-CTRP3 + 666-15 group.
666-15 potently inhibits cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI₅₀ for 666-15 is 73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibits robust activity as well with GI₅₀ of 0.47 and 0.31 μM. 666-15 is also found to be a rather weak inhibitor of CREB-CBP interaction with IC₅₀ of 18.27 μM. 666-15 inhibits CREB’s transcription activity in living cells independent of direct CREB or CBP binding interaction. 666-15 is very potent in inhibiting CREB’s transcription activity. 666-15 also inhibits endogenous CREB target gene expression, the transcript level of nuclear receptor related 1 protein (Nurr1/NR4A2).

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

Cell Proliferation Assay

Cell Line:	CTRL or MSN-overexpressing MDA-MB-231 cells
Concentration:	73 nM
Incubation Time:	For 12hours
Result:	Significantly blocked the cell proliferation caused by MSN overexpression.

Western Blot Analysis

Cell Line:	NRCMs
Concentration:	1 μM
Incubation Time:	2 hour (pretreated)
Result:	Effectively inhibited PE-induced CREB phosphorylation.

体内研究
(In Vivo)

666-15 (10 mg/kg; IP; once a week; for 11 weeks) alone can play a good role in inhibiting the growth of breast cancer, and the combination with RP-56976 (DOC) shows a better effect.

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

Animal Model:	1-month-old female nude mice with MDA-MB-231 or T47D cells
Dosage:	10 mg/kg
Administration:	IP; once a week; for 11 weeks
Result:	Played a good role in inhibiting the growth of breast cancer.

体内研究

666-15 (10 mg/kg; IP; once a week; for 11 weeks) alone can play a good role in inhibiting the growth of breast cancer, and the combination with RP-56976 (DOC) shows a better effect.

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

Animal Model:	1-month-old female nude mice with MDA-MB-231 or T47D cells
Dosage:	10 mg/kg
Administration:	IP; once a week; for 11 weeks
Result:	Played a good role in inhibiting the growth of breast cancer.

体内研究

666-15 (10 mg/kg; IP; once a week; for 11 weeks) alone can play a good role in inhibiting the growth of breast cancer, and the combination with RP-56976 (DOC) shows a better effect.

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

Animal Model:	1-month-old female nude mice with MDA-MB-231 or T47D cells
Dosage:	10 mg/kg
Administration:	IP; once a week; for 11 weeks
Result:	Played a good role in inhibiting the growth of breast cancer.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (201.44 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6116 mL	8.0578 mL	16.1155 mL
5 mM	0.3223 mL	1.6116 mL	3.2231 mL
10 mM	0.1612 mL	0.8058 mL	1.6116 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 (sealed storage, away from moisture)。-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: ≥ 2.08 mg/mL (3.35 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (3.35 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (3.35 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 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.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.35 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.35 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。