SCH529074|cas:922150-11-6|西域试剂

SCH529074,99.73%

产品编号：Bellancom-110088| CAS NO：922150-11-6| 分子式：C₃₁H₃₆Cl₂N₆| 分子量：563.56

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-110088	￥2000.00	杭州北京（现货）
Bellancom-110088	￥3500.00	杭州北京（现货）
Bellancom-110088	￥7000.00	杭州北京（现货）
Bellancom-110088	￥11000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

SCH529074

产品介绍

SCH529074 是一种具有口服活性的 p53 激活剂。SCH529074 与 p53 DBD 特异性结合并与构象相关，其 K_i值为 1-2 μM。SCH529074 恢复突变的 p53 功能，并阻断 HDM2 介导的野生型 p53 泛素化。SCH529074 可用于非小细胞肺癌 NSCLC 的研究。

生物活性

SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a K_i of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC).

体外研究

SCH529074 (2-4 µM; 24 hours) causes significant reduction in cell viability, it causes a significant decreasing to 20-25% in p53 mutant cells (H157, H1975 and H322) and to 68% in the p53 WT cell line A549 at 4 µM.
SCH 529074 (2 and 4 µM) induces NSCLC cells (H157, A549, HCT116 and HCT116 p53^-/-) arrested at the G0/G1 phase (59%; 72%; 66%; and 57%) compared with the control cells following low concentration (2 µM) of treatment.
SCH 529074 (2-4 µM; 24 hours) induces the early and late apoptotic rates at 2 µM in H1975 cells. In H157 cells, SCH 529074 treatment induces early and late apoptosis. Similarly, in A549 cells, 2 and 4 µM of SCH 529074 significantly increased early and late apoptosis. In line with that, in colon cancer cells, in HCT116 cells, 4 µM of SCH 529074 causes a significant induction of early and late apoptosis, and 4 µM of SCH 529074 significantly induces early apoptosis in HCT116 p53^-/- cells.
SCH 529074 (2-6 µM; 24 hours) increases the protein levels of PUMA and p21 revealed to 4 or 6 µM in the cancer cell lines regardless of their p53 status.

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

Cell Viability Assay

Cell Line:	p53 mutant cells (H157, H1975 and H322) and p53 WT cell line A549
Concentration:	2 µM; 4 µM
Incubation Time:	24 hours
Result:	Inhibited cancer WT and mutant cell viability.

Cell Cycle Analysis

Cell Line:	H1975, H157, A549, HCT116, HCT116 p53^-/- cells
Concentration:	2 µM, 4 µM, 6 µM
Incubation Time:	24 hours
Result:	Induced apoptosis in all assessed NSCLC cell lines irrespective of their p53 mutational status.

Western Blot Analysis

Cell Line:	H1975, H322, H157, A549, HCT116, HCT116 p53^-/-
Concentration:	2 µM, 4 µM, 6 µM
Incubation Time:	24 hours
Result:	Increased PUMA and p21 protein expression.

体内研究
(In Vivo)

SCH529074 (oral administration; 30 or 50 mg/kg; twice daily; 4 weeks; started on day 3 until day 31) causes 79 and 43% reduction of tumor growth at 50 and 30 mg/kg doses, respectively. the degree of tumor inhibition correlates with the plasma exposure of the compound (0.26–0.55 μm at 30 mg/kg and 0.39-0.79 μm at 50 mg/kg, 2-12 h post final dosing) in human DLD-1 colorectal cancer xenograft.

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

Animal Model:	Female nude mice, 5–7 weeks of age, received subcutaneous inoculation of DLD-1 human colorectal carcinoma cells
Dosage:	30 or 50 mg/kg
Administration:	Oral administration; twice daily; 4 weeks; started on day 3 until day 31
Result:	Inhibited tumor growth

体内研究

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

Animal Model:	Female nude mice, 5–7 weeks of age, received subcutaneous inoculation of DLD-1 human colorectal carcinoma cells
Dosage:	30 or 50 mg/kg
Administration:	Oral administration; twice daily; 4 weeks; started on day 3 until day 31
Result:	Inhibited tumor growth

体内研究

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

Animal Model:	Female nude mice, 5–7 weeks of age, received subcutaneous inoculation of DLD-1 human colorectal carcinoma cells
Dosage:	30 or 50 mg/kg
Administration:	Oral administration; twice daily; 4 weeks; started on day 3 until day 31
Result:	Inhibited tumor growth

性状

Solid

溶解性数据

In Vitro:

DMSO : 20 mg/mL (35.49 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7744 mL	8.8722 mL	17.7443 mL
5 mM	0.3549 mL	1.7744 mL	3.5489 mL
10 mM	0.1774 mL	0.8872 mL	1.7744 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: ≥ 1 mg/mL (1.77 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.77 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 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% corn oil
Solubility: ≥ 1 mg/mL (1.77 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.77 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 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。