2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK JAK/STAT Signaling PI3K/Akt/mTOR
  3. NEKs CDK Discoidin Domain Receptor EGFR PI3K
  4. AP4-43

AP4-43 是一种具有口服活性的 CLK1，CLK4，PI3K，DDR1，EGFR 和 NEK4 抑制剂。AP4-43 可抑制哺乳动物结直肠癌类器官的生长。AP4-43 可提高携带 KRAS 突变的结直肠癌转基因果蝇模型的存活率。AP4-43 可用于 KRAS 突变型结直肠癌的相关研究。

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AP4-43

AP4-43 Chemical Structure

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AP4-43 相关抗体

Top Publications Citing Use of Products

查看 NEKs 亚型特异性产品:

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NEK1 NEK2 NEK4 NEK6 NEK7

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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DDR1 DDR2

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AP4-43 is an orally active CLK1, CLK4, PI3K, DDR1, EGFR and NEK4 inhibitor. AP4-43 reduces growth of mammalian colorectal cancer organoids. AP4-43 improves survival in a transgenic Drosophila model of KRAS-mutant colorectal cancer. AP4-43 can be used for the research of KRAS-mutant colorectal cancer[1].

IC50 & Target[1]

CLK1

 

CLK4

 

NEK4

 

DDR1

 

体外研究
(In Vitro)

AP4-43 (10 pM-100 μM；72 小时) 可抑制由 KRAS 驱动的人结直肠癌细胞 SW620 的活力，其 IC50 为 2.23 µM；经 72 小时处理后，对 SW837 细胞的 IC50 为 15.41 µM[1]。
AP4-43 (2 µM) 比 2 µM Regorafenib (HY-10331) 更有效地抑制携带 KRAS 突变的 AKP 小鼠结直肠癌类器官的生长[1]。
AP4-43 (2 µM；24 小时) 可抑制 AKP 小鼠 KRAS 突变结直肠癌类器官中 CLK1 依赖的 Wnt/β-catenin 信号通路以及 CLK4 依赖的 NF-κB 激活，且不影响 PI3K-AKT 或 RAS-MAPK 通路的活性[1]。

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

AP4-43 相关抗体:

Cell Viability Assay[1]

Cell Line: SW620 and SW837 cell lines
Concentration: 10 pM; 100 pM; 1 nM; 10 nM; 100 nM; 1 μM; 10 μM; 100 μM
Incubation Time: 72 h
Result: Inhibited the viability of SW620 human KRAS-driven colorectal cancer cells and SW837 cells with IC50s of 2.23 µM and 15.41 µM, respectively.
体内研究
(In Vivo)

AP4-43 (1-100 µM；口服；培养基持续给药) 通过靶向包含 CLK1 和 NEK4 的多激酶网络，提升了患者匹配的黑腹果蝇结直肠癌模型的存活率；当与 NEK4 基因剂量降低联合使用时可观察到协同效应，在此情况下存活率可达 78.5%[1]。

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

Animal Model: Drosophila melanogaster (using byn-GAL4, UAS-GFP, GAL80ts and UAS-RAP-p1 transgenic lines; transgenic model expressing oncogenic RasG12V plus shRNAs targeting orthologues of human tumour suppressors Apc, P53, ago, wts, CG7742, and Atg2 in larval hindgut)[1]
Dosage: 1 µM; 10 µM; 100 µM
Administration: p.o.; continuous feeding in media
Result: Significantly improved byn>RAP-p1 survival over parent compound AP2-83 across multiple concentrations.
Reached 16.83% survival in byn>RAP-p1 flies at 10 µM alone.
Increased byn>RAP-p1; nek4-/+ fly survival to 78.5% (P < 0.0001) and caused significant reduction in hindgut proliferation zone area when combined with heterozygous loss of Drosophila NEK4 orthologue at 10 µM.
Improved survival in byn>RAP-p1; dyrk3-/+ flies when combined with heterozygous loss of CLK1 orthologue at 10 µM.
Did not improve survival in byn>RAP-p1; ddr-/+ flies at 10 µM.
Reduced survival in byn>RAP-p1; egfr-/+ flies at 10 µM.
分子量

382.18

Formula

C16H11BrF3N3
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

AP4-43 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

AP4-43NEKsCDKDiscoidin Domain ReceptorEGFRPI3KNIMA–related KinasesNIMA (never in mitosis gene a)-related Expressed KinasesCyclin dependent kinaseEpidermal growth factor receptorErbB-1HER1Phosphoinositide 3-kinasetransgenic DrosophilaDDR1mammalian colorectal cancer organoidsCLK4NEK4CLK1SW837 cellsSW620 human KRAS-driven colorectal cancer cellsKRAS-mutant colorectal cancerInhibitorinhibitorinhibit

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