LS-Q2
LS-Q2 is a highly selective CDK4/9 inhibitor with IC50 values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors.
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- 分子式: C26H35N7O
- 分子量:461.60
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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CDK4 1.4 nM (IC50) |
CDK9 6.2 nM (IC50) |
CDK6 52 nM (IC50) |
Aurora A 212 nM (IC50) |
CDK7 748 nM (IC50) |
CDK5 795 nM (IC50) |
CDK1 1249 nM (IC50) |
CDK2 1491 nM (IC50) |
CDK8 >10000 nM (IC50) |
LS-Q2 (Compound 6m) shows potent inhibitory activity against CDK4 and 9 with IC50 values of 1.4 and 6.2 nM, and shows weak inhibitory against CDK6 (IC50 = 52 nM), CDK1, 2, 5, 7, 8 (IC50 >700 nM)[1].
LS-Q2 inhibits tumor cell proliferation with in MIA Paca-2, HCT116, Hela cells with IC50 values of 0.62, 0.75, 2.77 μM[1].
LS-Q2 (0.5-2 μM; 24 h) induces G2/M phase arrest and apoptosis in HepG2 cells[1].
LS-Q2 (0.5-2 μM; 24 h) reduces pSer2 RNA polymerase II expression in HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:24 h
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Result:Reduced pSer2 RNA polymerase II, P-RB expression.
化学情報
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分子量 461.60
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分子式 C26H35N7O
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SMILES
CN(C(C1=CC2=C(N1C3CCCC3)N=C(N=C2)NC4=CC=C(C=C4)CN5CCCNCC5)=O)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)