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- 详细信息
- 文献和实验
- 技术资料
- 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:
883561-04-4
- 规格:
1 mg/5 mg/10 mg
| 规格: | 1 mg | 产品价格: | ¥1360.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥3000.0 |
| 规格: | 10 mg | 产品价格: | ¥4800.0 |
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CA224
CAS No. : 883561-04-4
MCE 国际站:CA224
产品活性:CA224 (Compound 1) 是一种选择性的、具有口服活性的 Cdk4–cyclin D1 抑制剂, IC50 值为 6.2 µM。CA224 诱导细胞凋亡 (apoptosis),具有抗肿瘤活性。
研究领域:Cell Cycle/DNA Damage | Apoptosis
In Vitro: CA224 (Compound 1) (48 h) shows antiproliferation activity against human cancer cell lines.
CA224 (18-48 h) blocks the growth of cancer cells at G0/G1 and G2/M phase of the cell cycle, and selectively kills SV40 large T-antigen transformed normal mouse embryonic liver cells (BNL SV A.8).
CA224 (0-4 µM, 30 min) inhibits tubulin polymerization and enhances the depolymerization of stabilized tubulin protein.
CA224 (0-72 h) induces cell apoptosis in cancer cells.
CA224 (10 μM) shows 50%, 14%, 51% and 19% inhibition of CYP3A4, CYP2D6, CYP2C9, and CYP2C19, respectively.
In Vivo: CA224 (Compound 1) (100 mg/kg; i.p.; once a day for 9 days) shows significant tumor growth inhibition without obvious toxicity.
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文献和实验,可根据加和性原则列出以下关系式:D663 = 82.04Ca+9.27Cb (1)D645 = 16.75Ca+45.60Cb (2)式(1)、(2)中的D663和D645为叶绿素溶液在波长663nm和645nm时的光密度,Ca、Cb分别为叶绿素a和b的浓度,以mg/L为单位。解方程组(1)、(2),得:Ca = 12.72D
(Araujo 等人, 2016 年; Sakaue-Sawano 等人, 2008 年)。 其中一种探针是基于荧光泛素化的细胞周期指示剂 FUCCI (CA),由 Miyawaki 及其同事开发(Sakaue-Sawano 等人, 2017 年),它监控 Cdt1 和联会蛋白(两种重要的细胞周期蛋白)的降解,产生 G1、S 和 G2 期(红色、绿色和黄色)的清晰三色分离,可在显微镜的 YFP 和 mCherry 通道中观察到(图 2)。 图 2. 使用 FUCCI(CA) 探针测量细胞周期的 G1
式中Kd为 Fura-2与Ca 结合反应的介离常数,37℃ 时其值为224nmol/L,Fmax是细胞内Fura-2全部为Ca 饱和时的荧光比值(采用Ca 载体),Fmin为Fura-2完全未结合Ca 时的荧光比值。通过向介质中加入过量的EGTA将细胞内外的游离Ca 螯合,此时测得的最小荧光值。F为实验中以340nm和380nm波长激发,500nm波长发射测定负载Fura-2/AM细胞的荧光比值。 静息态时[Ca ]i ]0 浓度为1~
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