LCI133
LCI133 is afirst-in-class,nanomolar-potent, selective multikinase inhibitor targeting CDK4/6/9 and AURKA/B (IC50 = 4.7/10.2/4.1 nM and 2.8/10.6 nM). LCI133 induces S/G2 cell-cycle arrest and robust apoptosis in MYCN-amplified neuroblastoma BE(2)-C cells. LCI133 demonstrates significant antitumor efficacy in a BE(2)-C neuroblastoma xenograft model.
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- CAS No.: 3065284-87-6
- Formule: C33H34N6O4
- Masse moléculaire:578.66
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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
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Activité biologique
|
CDK4 4.7 nM (IC50) |
CDK6 10.2 nM (IC50) |
CDK9 4.1 nM (IC50) |
Aurora A 2.8 nM (IC50) |
Aurora B 10.6 nM (IC50) |
LCI133 (72 h) reduces cell viability in BE(2)-C, NGP, Kelly, SK-N-AS and SHEP neuroblastoma cells (IC50 = 0.17-0.55 μM)[1].
LCI133 (0.5-1 μM; 24 h) induces cell-cycle arrest in BE(2)-C cells (S-phase increase with a pronounced G2 blockade)[1].
LCI133 (0.5-1 μM; 24 h) increases apoptosis in BE(2)-C cells (Annexin V/7-AAD)[1].
LCI133 (0.5-1 μM; 24 h) inhibits RNAP II Ser2 phosphorylation and decreases MCL-1 protein levels in BE(2)-C and NGP cells[1].
LCI133 (0.5-1 μM; 24 h) increases cleaved PARP in BE(2)-C cells[1].
LCI133 (0.5 μM; 3 h) decreases MYCN and MCL1 mRNA levels in BE(2)-C cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BE(2)-C
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Concentration:0.5 μM; 1 μM
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Incubation Time:24 h
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Result:Increased the proportion of cells in S phase at 1 μM.
Induced a pronounced G2-phase blockade at 0.5 μM and 1 μM.
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Cell Line:BE(2)-C
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Concentration:0.5 μM ; 1 μM
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Incubation Time:24 h
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Result:Increased apoptosis, as indicated by an increased proportion of Annexin V/7-AAD–positive cells.
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Cell Line:BE(2)-C ; NGP
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Concentration:0.5 μM; 1 μM
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Incubation Time:24 h
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Result:Inhibited RNAP II Ser2 phosphorylation and decreased MCL-1 protein levels in BE(2)-C and NGP cells.
Increased cleaved PARP in BE(2)-C cells.
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Cell Line:BE(2)-C
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Concentration:0.5 μM
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Incubation Time:3 h
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Result:Decreased MYCN (p = 0.006) and MCL1 (p < 0.0003) mRNA expression versus DMSO control.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult female NSG mice bearing subcutaneous BE(2)-C xenografts (1 × 10^6 cells injected s.c. into the right flank; 2-3 weeks engraftment)[1].
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Dosage:40 mg/kg/d
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Administration:Intraperitoneal injection (i.p.), once daily (QD), for 28 days.
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Result:Significantly reduced BE(2)-C xenograft tumor growth and improved overall survival without obvious changes in mouse behavior or body weight.
Chemical Information
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CAS No. 3065284-87-6
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Masse moléculaire 578.66
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Formule C33H34N6O4
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SMILES
CN(C(C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(C=C4)C5=CC6=C(C(C=C(O6)N7CCOCC7)=O)C=C5)=O)C
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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)
LCI133 Related Classifications
HY-179375 Related Classifications
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