製品番号: HY-183068

AP4-43

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Based on 1 Customer Validation

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.76%
分子式: C₁₆H₁₁BrF₃N₃
分子量:382.18

保管条件:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

AP4-43 構造式

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

CLK1

CLK4

NEK4

DDR1

NEKs アイソフォーム固有の製品をすべて表示 :

CDK アイソフォーム固有の製品をすべて表示 :

Discoidin Domain Receptor アイソフォーム固有の製品をすべて表示 :

DDR1
DDR2

EGFR アイソフォーム固有の製品をすべて表示 :

PI3K アイソフォーム固有の製品をすべて表示 :

体外実験

AP4-43 (10 pM-100 μM; 72 hr) inhibits the viability of SW620 human KRAS-driven colorectal cancer cells with an IC₅₀ of 2.23 µM and SW837 cells with an IC₅₀ of 15.41 µM^[1].
AP4-43 (2 µM) reduces the growth of AKP mouse KRAS-mutant colorectal cancer organoids more effectively than 2 µM Regorafenib (HY-10331)^[1].
AP4-43 (2 µM; 24 hr) inhibits CLK1-dependent Wnt/β-catenin signalling and CLK4-dependent NF-κB activation in AKP mouse KRAS-mutant colorectal cancer organoids, without affecting PI3K-AKT or RAS-MAPK pathway activity^[1].

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

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.

体内実験

AP4-43 (1-100 µM; p.o.; continuous feeding in media) enhances survival of a patient-matched Drosophila colorectal cancer model by targeting a multi-kinase network including CLK1 and NEK4, with synergistic efficacy observed when combined with reduced NEK4 gene dosage, reaching 78.5% survival in this context^[1].

MedChemExpress (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 Ras^G12V 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.

化学情報

性状 Solid
分子量 382.18
分子式 C₁₆H₁₁BrF₃N₃
SMILES

BrC1=CC2=C(NC3=CC=C(C)C(C(F)(F)F)=C3)N=CN=C2C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Badmos HA, et al. Chemical programming of kinase inhibitors in a modular chemputer-based system. Commun Biol. Published online March 27, 2026. [Content Brief]

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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AP4-43

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

NEKs アイソフォーム固有の製品をすべて表示

CDK アイソフォーム固有の製品をすべて表示

Discoidin Domain Receptor アイソフォーム固有の製品をすべて表示

EGFR アイソフォーム固有の製品をすべて表示

PI3K アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

AP4-43 関連分類

HY-183068 関連分類