ZLMT-72
ZLMT-72 is an orally active dual CDK2 and CDK9 inhibitor with IC50s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC).
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- 화학식: C29H32FN5O
- 분자량:485.60
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All DNA/RNA Synthesis Isoforms
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Biological Activity
|
RNA Polymerase |
CDK2/CycA2 0.741 (IC50) |
CDK9/CycT1 1.03 (IC50) |
Mcl-1 |
XIAP |
ZLMT-72 (1-10 nM; 10 days) completely suppresses colony formation in HCT116 cells[1].
ZLMT-72 (1-10 nM; 72 hours) demonstrates potent antiproliferative effects in HCT116 cells[1].
ZLMT-72 (1-10 nM; 48 hours) induces significant apoptosis in HCT116 cells[1].
ZLMT-72 (1-10 nM; 24 hours) significantly inhibits HCT116 cell migration[1].
ZLMT-72 (1-10 nM; 48 hours) inhibits CDK2/9 and reduces antiapoptotic protein expression in HCT116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:1 nM, 3.3 nM, 10 nM
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Incubation Time:72 hours
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Result:Exhibited potent antiproliferative effects, with GI50 values < 0.1 nM. The compound significantly inhibited cell proliferation.
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Cell Line:HCT116 cells
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Concentration:1 nM, 3.3 nM, 10 nM
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Incubation Time:10 days
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Result:Completely suppressed colony formation in HCT116 cells at 10 nM, demonstrating strong antiproliferative activity.
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Cell Line:HCT116 cells
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Concentration:10 nM, 3.3 nM, 1 nM
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Incubation Time:48 hours
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Result:Induced apoptosis in 30.19% of HCT116 cells at 10 nM, with 23.3% early-stage and 6.89% late-stage apoptosis.
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Cell Line:HCT116 cells
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Concentration:1 nM, 3.3 nM, 10 nM
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Incubation Time:24 hours
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Result:Significantly inhibited HCT116 cell migration at 10 nM and 3.3 nM, with a reduced migration rate.
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Cell Line:HCT116 cells
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Concentration:10 nM, 3.3 nM, 1 nM
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Incubation Time:48 hours
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Result:Significantly downregulated the levels of phosphorylated Rb (p-Rb) and inhibited the phosphorylation of RNA polymerase II at the Ser2 site, indicating CDK2/9 inhibition.
Also reduced the expression of antiapoptotic proteins (MCL-1 and XIAP).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c nude mice bearing HCT116 cells (subcutaneous and orthotopic xenograft tumor models)[1]
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Dosage:10 mg/kg, 3.3 mg/kg, 1.1 mg/kg
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Administration:Oral, oral, twice daily, for 14 days
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Result:Tumor growth was significantly inhibited in both subcutaneous and orthotopic models.
At 10 mg/kg, tumor growth inhibition (TGI) was 50.6% in subcutaneous models and 84.3% in orthotopic models.
Revealed a significantred reduction in Ki67-positive and CDK20-positive cells.
Tumor weight and volume were significantly reduced, and no significant toxicity was observed.
Chemical Information
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분자량 485.60
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화학식 C29H32FN5O
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SMILES
O=C([C@@H]1[C@@H](F)C1)NC2=CC(C3=CC=C(N=C(CCCCC4)C4=C5N6C[C@@H](CNC7)[C@@H]7C6)C5=C3)=CC=N2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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