SCH529074 is a potent and orally activep53activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with aK_iof 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)^[1][2].

Ki: 1-2 μM (p53 DBD)^[2]

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

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^[2].

563.56

Solid

C₃₁H₃₆Cl₂N₆

922150-11-6

Room temperature in continental US; may vary elsewhere.

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

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。

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。