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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
922150-11-6
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2200.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥909.0 |
| 规格： | 5 mg | 产品价格： | ￥2000.0 |
| 规格： | 10 mg | 产品价格： | ￥3500.0 |
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SCH529074
CAS No. : 922150-11-6
MCE 国际站：SCH529074
产品活性：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 Ki 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。
研究领域：Apoptosis
作用靶点：MDM-2/p53
In Vitro: 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.
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.
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文献和实验疟原虫 Malaria Parasites(Plasmodium)
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在植物生长发育期，要经过 4-11个月旱季的地方所见到的植物群落。叶子退化，由枝、茎较粗，且有叶绿素的耐旱性很强的高树〔有刺高树林（德 Dorn-wald）〕或矮丛林〔有刺低丛林（德 Dorngobüsch）〕组成。有时会把具同样生活型的草本植物混淆在一起。多出现在稀树干草原和干燥荒原间的干燥气候地带。分布在非洲南部和东部〔金合欢（ Acacia）、阿当屯（ Adenia）、大戟（ Euphorbia）〕、澳大利亚南部〔火烟树（ Brachychiton）〕、南美的秘鲁和智利
c 11 13 14 16 18 20 Water d 5.81 ml 5.07 ml 4.7 ml 3.95 ml 3.21 ml 2.47 ml Heavy gel buffer 5 ml 5 ml 5 ml 5 ml 5 ml 5 ml Gel A/B 3.72 ml 4.40 ml 4.74 ml 5.41 ml 6.09 ml 6.77 ml Gel A 404 µl 478 µl 514 µl
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