2. Cell Cycle/DNA Damage Apoptosis
  3. Wee1 Apoptosis
  4. APO-50815

APO-50815 是一种 WEE1 激酶抑制剂，对人源的 IC50 为 9 nM。APO-50815 可诱导 DNA 损伤、复制应激、S 期细胞累积和细胞凋亡 (apoptosis)。APO-50815 可用于转移性结直肠癌的研究。

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APO-50815

APO-50815 Chemical Structure

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APO-50815 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

APO-50815 is a WEE1 kinase inhibitor with a human IC50 of 9 nM. APO-50815 induces DNA damage, replication stress, S-phase cell accumulation, and apoptosis. APO-50815 can be used for the research of metastatic colorectal cancer[1].

体外研究
(In Vitro)

APO-50815 (Compound 14) 可强效抑制重组人 WEE1 激酶，其 IC50 为 9 nM，对 WEE1 的选择性比对 PLK1 高 10 倍，且在浓度高达 10 μM 时对 CHK1 无活性[1]。
APO-50815 (100 pM-100 μM；5 天) 可强效降低 TP53 突变型腹膜转移性结直肠癌类器官系 PM003 (IC50 = 37 nM) 和 PM025 (IC50 = 74 nM) 的存活率，其疗效优于临床及临床前阶段的 WEE1 抑制剂[1]。
APO-50815 (100 pM-100 μM；5 天) 可强效降低 TP53 突变型肝转移结直肠癌类器官细胞系 QEH039LM 的存活率 (IC50 = 50 nM)，并对 KRASG12X_ 突变、WEE1 抑制剂耐药的细胞系 QEH042LM 表现出更强的活性 (IC50 = 633 nM)，其疗效优于临床用 WEE1 抑制剂[1]。
APO-50815 (100 pM-100 μM；5 天) 可强效且选择性地降低具有不同突变谱的原代 CRC 类器官的活力，其治疗指数分别为 238 (RAH051)、146 (RAH035) 和 129 (RAH057)[1]。
APO-50815 (300 nM；48 小时) 可显著减少 TP53-野生型、BRAFV600E 结直肠癌原代类器官株 RAH051T 中的活跃周期进程，放大 DNA 损伤并增加 S 期细胞积累，同时增强细胞凋亡[1]。
APO-50815 (90 nM；2 小时) 可显著降低 MDA-MB-231HM 细胞中 pTyr15-CDK1 的水平，证实其可在细胞内与 WEE1 靶点结合并对其产生功能性抑制作用[1]。
APO-50815 (1 μM) 在人源和小鼠肝微粒体中的代谢稳定性较差，其半衰期短、固有清除率高，表明代谢速度快[1]。

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

APO-50815 相关抗体:

Cell Viability Assay[1]

Cell Line: CRC organoid lines PM003 and PM025; TP53-mutated liver metastatic CRC organoid line QEH039LM; primary CRC organoids
Concentration: 0.1 nM; 1 nM; 10 nM; 100 nM; 1 μM; 10 μM; 100 μM
Incubation Time: 5 days
Result: Potently reduced viability of TP53-mutated peritoneal metastatic CRC organoid lines PM003 (IC50 = 37 nM) and PM025 (IC50 = 74 nM).
Potently reduced viability of TP53-mutated liver metastatic CRC organoid line QEH039LM (IC50 = 50 nM) and exhibited enhanced activity against the KRASG12X-mutated, WEE1 inhibitor-resistant line QEH042LM (IC50 = 633 nM).
Potently and selectively reduced viability of primary CRC organoids across diverse mutation profiles, with exceptional therapeutic indices of 238 (RAH051), 146 (RAH035), and 129 (RAH057).

Cell Cycle Analysis[1]

Cell Line: TP53-WT, BRAFV600E primary CRC organoid line RAH051T
Concentration: 300 nM
Incubation Time: 48 h
Result: Significantly reduced active cycling, amplified DNA damage and S phase accumulation, and enhanced apoptosis.

Western Blot Analysis[1]

Cell Line: TP53-mutated MDA-MB-231HM triple negative breast cancer cells
Concentration: 90 nM
Incubation Time: 2 h
Result: Significantly reduced levels of pTyr15-CDK1, confirming functional inhibition of WEE1 activity and successful cell membrane permeation to engage the target.
分子量

527.64

Formula

C28H29N7O2S
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

APO-50815 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

APO-50815APO50815APO 50815Wee1Apoptosisreplication stressWEE1 kinaseapoptosisMDA-MB-231HM cellspatient-derived organoidsCDK1 Tyr15 phosphorylationmetastatic colorectal cancerliver microsomesDNA damagecolorectal cancerInhibitorinhibitorinhibit

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目录号：
HY-183278
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