TD52|cas:1798328-24-1|西域试剂

TD52,95.0%

产品编号：Bellancom-135699| CAS NO：1798328-24-1| 分子式：C₂₄H₁₆N₄| 分子量：360.41

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-135699	￥1200.00	杭州北京（现货）
Bellancom-135699	￥2100.00	杭州北京（现货）
Bellancom-135699	￥4200.00	杭州北京（现货）
Bellancom-135699	￥7200.00	杭州北京（现货）
Bellancom-135699	￥12500.00	杭州北京（现货）

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TD52

产品介绍

TD52 是 Erlotinib (HY-50896) 衍生物，一种具有口服活性的强效癌性蛋白磷酸酶 2A (CIP2A) 抑制剂。TD52 通过调节 CIP2A/PP2A/p-Akt 信号通路介导三阴性乳腺癌 (TNBC) 细胞的凋亡作用。TD52 通过干扰 Elk1 与 CIP2A 启动子的结合间接减少 CIP2A。TD52 具有小的 p-EGFR 抑制作用并具有抗癌活性。

生物活性

TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity.

体外研究

TD52 (2-10 μM; 48 hours) shows anti-proliferative ability and induces differential apoptotic effects in these cell lines.
TD52 (5 μM; 48 hours) has minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression.
TD52 (2.5, 5, 7.5 μM; 48 hours) time-dependently induces apoptosis accompanied with downregulating CIP2A and p-Akt.
TD52 (5 μM; 24 hours) significantly increases the phosphatase activity of PP2A in TNBC cells.
TD52 (5 μM; 48 hours) has no obvious effects on other common RTKs, such as IGFR, PDGFR and VEGFR2.

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

Apoptosis Analysis

Cell Line:	Three TNBC cell lines including HCC-1937, MDA-MB-231 and MDA-MB-468 cells
Concentration:	2, 4, 6, 8, 10 μM
Incubation Time:	48 hours
Result:	Showed anti-proliferative ability and induced differential apoptotic effects in these cell lines.

Western Blot Analysis

Cell Line:	MDA-MB-231 cell
Concentration:	5 μM
Incubation Time:	48 hours
Result:	Had minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression.

体内研究
(In Vivo)

TD52 (10 mg/kg/day; oral gavage; for 52 days) significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight.

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

Animal Model:	Female NCr athymic nude mice (5-7 weeks of age)
Dosage:	10 mg/kg
Administration:	Oral gavage; daily; for 52 days
Result:	Significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight. Decreased the protein expressions of CIP2A and p-Akt in the three MDA-MB-468 xenograft tumours.

体内研究

TD52 (10 mg/kg/day; oral gavage; for 52 days) significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight.

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

Animal Model:	Female NCr athymic nude mice (5-7 weeks of age)
Dosage:	10 mg/kg
Administration:	Oral gavage; daily; for 52 days
Result:	Significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight. Decreased the protein expressions of CIP2A and p-Akt in the three MDA-MB-468 xenograft tumours.

体内研究

TD52 (10 mg/kg/day; oral gavage; for 52 days) significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight.

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

Animal Model:	Female NCr athymic nude mice (5-7 weeks of age)
Dosage:	10 mg/kg
Administration:	Oral gavage; daily; for 52 days
Result:	Significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight. Decreased the protein expressions of CIP2A and p-Akt in the three MDA-MB-468 xenograft tumours.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (277.46 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7746 mL	13.8731 mL	27.7462 mL
5 mM	0.5549 mL	2.7746 mL	5.5492 mL
10 mM	0.2775 mL	1.3873 mL	2.7746 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 (6.94 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.94 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 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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.94 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.94 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 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