2. Cell Cycle/DNA Damage
  3. CDK
  4. Anticancer agent 299

Anticancer agent 299 (compound P12) 是一种细胞周期抑制剂、衰老诱导剂、凋亡诱导剂和抗增殖剂。Anticancer agent 299 对癌细胞表现出选择性活性，在相关浓度下对非肿瘤软骨细胞的影响极小。Anticancer agent 299 可用于 ER+/HER2− 乳腺癌和 BRAF 突变型黑色素瘤的研究。

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Anticancer agent 299

Anticancer agent 299 Chemical Structure

CAS No. : 1414873-26-9

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Anticancer agent 299 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anticancer agent 299 (compound P12) is a cell-cycle inhibitor, senescence inducer, apoptosis inducer, and antiproliferative agent. Anticancer agent 299 exhibits selective activity against cancer cells with minimal effects on non-tumoral chondrocyte cells at relevant concentrations. Anticancer agent 299 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma[1].

体外研究
(In Vitro)

Anticancer agent 299 (P12)(5-50 μM；作用 7 天) 可降低 MCF7 和 A375 细胞的集落形成能力，其 IC50值分别为 30.22 μM 和 2.915 μM，且在 5-35 μM 浓度下对非肿瘤细胞 TC28a2 的影响极小[1]。
抗癌剂 Anticancer agent 299 (P12) (5 μM；MCF7 细胞处理 12 天，A375 细胞检测 4 天) 可在处理 8 天和 12 天后缩小 MCF7 细胞的球状体面积，并在处理 4 天后缩小 A375 细胞的球状体面积[1]。
Anticancer agent 299 (P12)(5 μM；处理 7 天) 可将 MCF7 细胞的 G2/M 期细胞比例降至 15.65%，将 A375 细胞的 G2/M 期细胞比例降至 1.94%[1]。
Anticancer agent 299 (P12) (5 μM；作用 7 天) 可上调 MCF7 细胞中 G1/S 及 S 期进入相关基因的表达，同时下调 A375 细胞中上述基因的表达[1]。
Anticancer agent 299 (P12)(5 μM；作用 7 天) 可上调 MCF7 和 A375 细胞中衰老相关基因 (p21、p53、IGFBP3、GDF15) 的表达[1]。
Anticancer agent 299 (P12) (5 μM；7 天) 可在MCF7细胞中上调 SASP 因子 (IL-6、IL-8)，但在 A375 细胞中无此作用[1]。
Anticancer agent 299 (P12) (作用时长≥4 天) 可诱导 MCF7 和 A375 细胞发生早期凋亡[1]。

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

Anticancer agent 299 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MCF7, A375, TC28a2
Concentration: 5, 20, 35, 50 μM (MCF7, A375 colony formation); 5, 20, 35, 50 μM (TC28a2 viability assay)
Incubation Time: 7 days
Result: Significantly reduced the colony-forming capacity of MCF7 and A375 cells in a dose-dependent manner. Achieved an IC50 of 30.22 μM in MCF7 cells and 2.915 μM in A375 cells. Did not produce a significant reduction in the number of adherent viable cells in non-tumoral TC28a2 cells from 5 to 35 μM.

Cell Proliferation Assay[1]

Cell Line: MCF7, A375
Concentration: 5 μM
Incubation Time: 12 days (MCF7 treatment); 4 days (A375 measurement)
Result: Significantly reduced spheroid area of MCF7 cells compared with the untreated control after 8 and 12 days of treatment. Significantly reduced spheroid size of A375 cells after 4 days of culture.

Cell Cycle Analysis[1]

Cell Line: MCF7, A375
Concentration: 5 μM
Incubation Time: 7 days
Result: Reduced the proportion of G2/M phase cells to 15.65% in MCF7 cells (vs. 26.25% untreated) and to 1.94% in A375 cells (vs. 5.44% untreated).

Real Time qPCR[1]

Cell Line: MCF7, A375
Concentration: 5 μM
Incubation Time: 7 days
Result: Significantly upregulated genes associated with G1/S transition and S-phase entry in MCF7 cells. Significantly downregulated key regulators of the G1/S transition and S-phase entry, including CCND1, CDK4, CDK6, and CCNE1, in A375 cells.\nInduced a notable increase in the expression of senescence-associated factors, including p21, p53, IGFBP3, and GDF15, in both MCF7 and A375 cells.\nSignificantly upregulated classical SASP components including IL-6 and IL-8 in MCF7 cells. Did not induce SASP factor expression and showed a trend toward reduced synthesis in A375 cells.
分子量

435.44

Formula

C25H20F3N3O
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

Anticancer agent 299 相关分类

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Keywords:

Anticancer agent 2991414873-26-9Anticancer agent299Anticancer agent-299CDKCyclin dependent kinaseCDK4A375 cellsCyclin E1BRAF-mutant melanomaMCF7 cellsCyclin D1ER+/HER2? breast cancerp21TC28a2 cellsCDK6Inhibitorinhibitorinhibit

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