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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- Formule: C28H29N7O2S
- Masse moléculaire:527.64
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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Cell Line:CRC organoid lines PM003 and PM025; TP53-mutated liver metastatic CRC organoid line QEH039LM; primary CRC organoids
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Concentration:0.1 nM; 1 nM; 10 nM; 100 nM; 1 μM; 10 μM; 100 μM
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Incubation Time:5 days
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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).
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Cell Line:TP53-WT, BRAFV600E primary CRC organoid line RAH051T
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Concentration:300 nM
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Incubation Time:48 h
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Result:Significantly reduced active cycling, amplified DNA damage and S phase accumulation, and enhanced apoptosis.
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Cell Line:TP53-mutated MDA-MB-231HM triple negative breast cancer cells
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Concentration:90 nM
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Incubation Time:2 h
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Result:Significantly reduced levels of pTyr15-CDK1, confirming functional inhibition of WEE1 activity and successful cell membrane permeation to engage the target.
Chemical Information
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Masse moléculaire 527.64
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Formule C28H29N7O2S
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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