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Ro-3306

CAS号

872573-93-8

分子式

C18H13N3OS2

主要靶点

PKC|CDK|PKA|Apoptosis|SGK|ERK

仅限科研使用

Cat No : CM03402

Print datasheet

Synonyms

Apoptosis|CDK|CDK1|Cyclin dependent kinase|ERK|Inhibitor|inhibit|Ro 3306|PKCδ|PKA|SGK|Ro3306|Ro-3306

验证数据展示

  • CAS No.: 872573-93-8

    Ro-3306
    CAS#: 872573-93-8

产品信息

CAS号 872573-93-8
分子式 C18H13N3OS2
主要靶点 PKC|CDK|PKA|Apoptosis|SGK|ERK
主要通路 蛋白酪氨酸激酶|细胞周期|细胞骨架|表观遗传|MAPK 信号通路|凋亡|代谢
分子量 351.45
纯度 99.74%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Apoptosis|CDK|CDK1|Cyclin dependent kinase|ERK|Inhibitor|inhibit|Ro 3306|PKCδ|PKA|SGK|Ro3306|Ro-3306

靶点活性

SGK:497 nM(Ki)|ERK:1980 nM(Ki)|PKCδ:318 nM(Ki)|CDK1:20 nM(Ki)

体内活性

方法：为检测体内抗肿瘤活性，将 Ro 3306 (4 mg/kg) 和 Cisplatin (4 mg/kg) 腹腔注射给携带卵巢癌肿瘤 OVCAR-3 的 BALB/c nude 小鼠，每四天一次，持续四周。 结果：与 Ro 3306 或 Cisplatin 治疗相比，联合治疗有效抑制了肿瘤生长。[1]

体外活性

方法：卵巢癌细胞 OVCA-429 和 OVCAR-3 用 Ro 3306 (1-2.5 nM) 处理 9 天，使用 crystal violet assay 检测细胞活力。 结果：OVCA-429 和 OVCAR-3 细胞在高剂量浓度的 Ro 3306 下长达 9 天的生长速率较低。使用 2.5 μM Ro 3306 处理，OVCA-429 和 OVCAR-3 细胞的生长率在第 9 天分别降低了 75.3% 和 87.7%。[1] 方法：人肿瘤细胞系 HCT116、SW480 和 HeLa 用 Ro 3306 (9 μM) 处理 20 h，使用 Flow cytometry 检测细胞周期。 结果：用 Ro 3306 对增殖的人类肿瘤细胞处理 20 h 导致 G2/M 期细胞周期的完全阻断。[2]

溶解度

DMSO:12.5 mg/mL (35.57 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1.25 mg/mL (3.56 mM)

细胞实验

Log phases cells (25,000) are seeed in 96-well plates and incubated in a 37℃ incubator with CO2, After 24 h, different concentrations of RO-3306 are administered to determine the drug concentrations required to achieve a 50% growth inhibition (IC50). MTT (20 μL, 5 mg/mL stock solution in saline) is added to each well and the cells are incubated for 4 h. Supernatants are removed and formazan crystals from viable cells are solubilized with 200 μL anhydrous DMSO. The absorbance is detected with a 550 model microplate reader at the 565 nm wavelength.(Only for Reference)

参考文献

1.Yang W, et al. Accumulation of cytoplasmic Cdk1 is associated with cancer growth and survival rate in epithelial ovarian cancer. Oncotarget. 2016 Aug 2;7(31):49481-49497.
2.Vassilev LT, et al. Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1. Proc Natl Acad Sci U S A. 2006 Jul 11;103(28):10660-5.
3.Xia Q, et al. Int J Oncol. 2014, 44(3), 735-744.
4.Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity[J]. Biochemical and biophysical research communications. 2019 Jun 11;513(4):967-973.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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C1   V1   C2   V2