2. Cell Cycle/DNA Damage Epigenetics
  3. CDK Aurora Kinase
  4. 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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LCI133

LCI133 Chemical Structure

CAS No. : 3065284-87-6

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LCI133 Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Aurora Kinase Aurora A Aurora B Aurora C

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Description

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[1].

IC50 & Target[1]

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)

In Vitro

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.

LCI133 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: BE(2)-C
Concentration: 0.5 μM; 1 μM
Incubation Time: 24 h
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.

Apoptosis Analysis[1]

Cell Line: BE(2)-C
Concentration: 0.5 μM ; 1 μM
Incubation Time: 24 h
Result: Increased apoptosis, as indicated by an increased proportion of Annexin V/7-AAD–positive cells.

Western Blot Analysis[1]

Cell Line: BE(2)-C ; NGP
Concentration: 0.5 μM; 1 μM
Incubation Time: 24 h
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.

RT-PCR[1]

Cell Line: BE(2)-C
Concentration: 0.5 μM
Incubation Time: 3 h
Result: Decreased MYCN (p = 0.006) and MCL1 (p < 0.0003) mRNA expression versus DMSO control.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-∞ AUC Vz-F_obs CL/F AUC0-last F
Mice[1] 2 mg/kg i.v. 2.8 h 0.1 h 3694.6 ng/mL 2791.8 ng·h/mL 0.1 % 3.0 L/kg 0.7 L/h/kg 2789.4 ng·h/mL /
Mice[1] 20 mg/kg p.o. 4.6 h 0.9 h 3305.3 ng/mL 7812.7 ng·h/mL 4.4 % 17.7 L/kg 2.6 L/h/kg 7480.5 ng·h/mL 28.9 %
In Vivo

LCI133-HCl (40 mg/kg/day; i.p.; QD; 28 days) significantly reduces tumor growth and improves overall survival in female NSG mice bearing subcutaneous BE(2)-C xenografts without overt toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage: 40 mg/kg/d
Administration: Intraperitoneal injection (i.p.), once daily (QD), for 28 days.
Result: Significantly reduced BE(2)-C xenograft tumor growth and improved overall survival without obvious changes in mouse behavior or body weight.
Molecular Weight

578.66

Formula

C33H34N6O4
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LCI133 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LCI1333065284-87-6LCI 133LCI-133CDKAurora KinaseCyclin dependent kinaseCDK4CDK6CDK9Aurora AAurora Bmultikinase inhibitorneuroblastomaMYCNMCL-1BE(2)-C xenograftInhibitorinhibitorinhibit

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