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

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.

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APO-50815

APO-50815 Chemical Structure

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APO-50815 Related Antibodies

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Description

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].

In Vitro

APO-50815 (Compound 14) potently inhibits recombinant human WEE1 kinase with an IC50 of 9 nM, exhibits 10-fold selectivity for WEE1 over PLK1, and is inactive against CHK1 at concentrations up to 10 μM[1].
APO-50815 (100 pM-100 μM; 5 days) potently reduces viability of TP53-mutated peritoneal metastatic CRC organoid lines PM003 (IC50 = 37 nM) and PM025 (IC50 = 74 nM), with superior efficacy compared to clinical and preclinical WEE1 inhibitors[1].
APO-50815 (100 pM-100 μM; 5 days) potently reduces viability of TP53-mutated liver metastatic CRC organoid line QEH039LM (IC50 = 50 nM) and exhibits enhanced activity against the KRASG12X-mutated, WEE1 inhibitor-resistant line QEH042LM (IC50 = 633 nM), outperforming clinical WEE1 inhibitors[1].
APO-50815 (100 pM-100 μM; 5 days) potently and selectively reduces viability of primary CRC organoids across diverse mutation profiles, with exceptional therapeutic indices of 238 (RAH051), 146 (RAH035), and 129 (RAH057)[1].
APO-50815 (300 nM; 48 h) significantly reduces active cycling, amplifies DNA damage and S phase accumulation, and enhances apoptosis in TP53-WT, BRAFV600E primary CRC organoid line RAH051T[1].
APO-50815 (90 nM; 2 h) significantly reduces pTyr15-CDK1 levels in MDA-MB-231HM cells, confirming intracellular WEE1 target engagement and functional inhibition[1].
APO-50815 (1 μM; up to 60 min at 37 °C) has poor metabolic stability in human and mouse liver microsomes, with short half-lives and high intrinsic clearances indicating rapid metabolism[1].

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

APO-50815 Related Antibodies

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.
Molecular Weight

527.64

Formula

C28H29N7O2S
SMILES

C=CCN1C(C2=CN=C(N=C2N1C3=CC=CC(C4(CSC4)O)=N3)NC5=CC6=C(C7(CN(C6)C)CC7)C=C5)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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APO-50815 Related Classifications

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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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