1. Cell Cycle/DNA Damage Apoptosis
  2. Wee1 Apoptosis
  3. PD-166285

PD-166285 是一种 PKMYT1 抑制剂,其 IC50 值为 17 nM。 PD-166285 对 CCNE1 扩增的 OVCAR3 细胞 (IC50 = 0.14 μM) 和 HCC1569 细胞 (IC50 = 0.21 μM) 表现出强烈的抗增殖作用。 PD-166285 可诱导细胞凋亡 (apoptosis),并使 CCNE1 扩增的 HCC1569 细胞阻滞于细胞周期的 G1/S 期。 PD-166285 可用于 PKMYT1 靶向 CCNE1 扩增癌症的研究。

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PD-166285

PD-166285 Chemical Structure

CAS No. : 717094-37-6

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生物活性

PD-166285 is a PKMYT1 inhibitor, with an IC50 value of 17 nM. PD166285 shows strong antiproliferative effects against CCNE1-amplified OVCAR3 cells (IC50 = 0.14 μM) and HCC1569 cells (IC50 = 0.21 μM). PD166285 induces apoptosis and arrests CCNE1-amplified HCC1569 cells at the G1/S phase of the cell cycle. PD166285 can be used for the research of PKMYT1-targeted therapies for CCNE1-amplified cancers[1].

IC50 & Target[1]

PKMYT1

17 nM (IC50)

体外研究
(In Vitro)

PD166285 (0.062-1 μM,5 天) 在 CCNE1 扩增的 OVCAR3 细胞 (IC50 = 0.14 μM) 和 HCC1569 细胞 (IC50 = 0.21 μM) 中表现出显著的抗增殖作用[1]
PD166285 (14 天) 以浓度依赖性方式抑制 CCNE1 扩增的 OVCAR3 细胞 (EC50 = 0.06 μM) 和 HCC1569 细胞 (EC50 = 0.16 μM) 的集落形成[1]
PD166285 (0.125-1 μM,5 天) 可诱导凋亡,并使 CCNE1 扩增的 HCC1569 细胞阻滞于细胞周期的 G1/S 期[1]

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

Cell Cycle Analysis[1]

Cell Line: CCNE1-amplified HCC1569 cells
Concentration: 0.125, 0.25, 0.5 μM
Incubation Time: 5 days
Result: Arrested CCNE1-amplified HCC1569 cells at the G1/S phase of the cell cycle.

Apoptosis Analysis[1]

Cell Line: CCNE1-amplified HCC1569 cells
Concentration: 0.125, 0.25, 0.5, 1 μM
Incubation Time: 5 days
Result: Induced apoptosis in CCNE1-amplified HCC1569 cells.
分子量

484.38

Formula

C24H23Cl2N5O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PD-166285
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HY-175819
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