PKMYT1-IN-10
PKMYT1-IN-10 is a selective PKMYT1 inhibitor with an IC50 of 3 nM. PKMYT1-IN-10 inhibits colony formation, induces apoptosis, and induces S-phase cancer cell cycle arrest. PKMYT1-IN-10 exhibits liver microsomal stability, favorable plasma stability, minimal CYPs inhibition. PKMYT1-IN-10 can be used for the studies of ovarian cancer and breast cancer.
For research use only. We do not sell to patients.
- Formula: C22H23N5O4S
- Molecular Weight:453.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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PKMYT1 3 nM (IC50) |
PKMYT1-IN-10 (Compound A30) demonstrates potent cytostatic activity, with IC50 values of 0.32 μM, 0.33 μM, and > 8 μM in the OVCAR3, HCC1569 and A549 cell lines, respectively[1].
PKMYT1-IN-10 (0.125-2 μM, 14 days) inhibits colony formation in the OVCAR3 and HCC1569 cells with EC50s of 0.37 and 0.35 μM[1].
PKMYT1-IN-10 (0.3-2.4 μM, 5 days) induces HCC1569 cells apoptosis and induces S-phase-specific cell cycle arrest in HCC1569 cells and OVCAR3 cells[1].
PKMYT1-IN-10 (37.5-600 nM) shows a high degree of synergy with Gemcitabine (HY-17026) with combination index (CI) values of < 0.5 and 0.5-0.8 in HCC1569 cells and OVCAR3 cells, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCC1569 cells
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Concentration:0.3, 0.6 and 1.2 μM
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Incubation Time:5 days
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Result:Reached the apoptosis rate by 54.7% at a concentration of 2.4 μM in HCC1569 cells.
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Cell Line:HCC1569 cells and OVCAR3 cells
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Concentration:0.3, 0.6 and 1.2 μM
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Incubation Time:5 days
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Result:Increased the proportion of cells in the S phase, without causing the typical G2/M arrest.
Chemical Information
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Molecular Weight 453.51
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Formula C22H23N5O4S
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SMILES
O=C(C1=CN=C(NC2=CC=C(S(=O)(C3CC3)=O)C=C2)N=C1N)NC4=C(C)C=CC(O)=C4C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)