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LCI133
Catalog No. T214195 Copy Product Info
🥰Excellent
LCI133 is an innovative, highly potent, and selective multi-target kinase inhibitor effective at the nanomolar level. It targets CDK4/6/9 and AURKA/B with IC50 values of 4.7/10.2/4.1 nM and 2.8/10.6 nM, respectively. In MYCN-amplified neuroblastoma BE(2)-C cells, LCI133 induces S/G2 phase arrest and triggers significant apoptosis (apoptosis). Moreover, LCI133 demonstrates substantial antitumor efficacy in BE(2)-C neuroblastoma xenograft models.
LCI133
Copy Product Info🥰Excellent
Catalog No. T214195
LCI133 is an innovative, highly potent, and selective multi-target kinase inhibitor effective at the nanomolar level. It targets CDK4/6/9 and AURKA/B with IC50 values of 4.7/10.2/4.1 nM and 2.8/10.6 nM, respectively. In MYCN-amplified neuroblastoma BE(2)-C cells, LCI133 induces S/G2 phase arrest and triggers significant apoptosis (apoptosis). Moreover, LCI133 demonstrates substantial antitumor efficacy in BE(2)-C neuroblastoma xenograft models.
LCI133
Cas No. 3065284-87-6
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | LCI133 is an innovative, highly potent, and selective multi-target kinase inhibitor effective at the nanomolar level. It targets CDK4/6/9 and AURKA/B with IC50 values of 4.7/10.2/4.1 nM and 2.8/10.6 nM, respectively. In MYCN-amplified neuroblastoma BE(2)-C cells, LCI133 induces S/G2 phase arrest and triggers significant apoptosis (apoptosis). Moreover, LCI133 demonstrates substantial antitumor efficacy in BE(2)-C neuroblastoma xenograft models. |
| Targets&IC50 | CDK4:4.7 nM |
| In vitro | LCI133 reduces cell viability in neuroblastoma cell lines BE(2)-C, NGP, Kelly, SK-N-AS, and SHEP with an IC50 range of 0.17-0.55 μM over 72 hours. It induces cell cycle arrest in S phase, with prominent G2 phase arrest, in BE(2)-C cells at concentrations of 0.5-1 μM over 24 hours. LCI133 also enhances apoptosis (Annexin V/7-AAD) in BE(2)-C cells at the same concentrations and duration. Additionally, it inhibits RNAP II Ser2 phosphorylation and decreases MCL-1 protein levels in BE(2)-C and NGP cells. In BE(2)-C cells, LCI133 increases cleaved PARP levels at 0.5-1 μM over 24 hours. Furthermore, LCI133 reduces MYCN and MCL1 mRNA expression levels in BE(2)-C cells at 0.5 μM over 3 hours. |
| In vivo | LCI133-HCl (40 mg/kg/day; i.p.; QD; 28 days) significantly inhibits the growth of BE(2)-C xenograft tumors in female NSG mice and improves overall survival without evident toxicity. |
| Molecular Weight | 578.67 |
| Formula | C33H34N6O4 |
| Cas No. | 3065284-87-6 |
| Smiles | O=C1C=C(OC2=CC(=CC=C12)C=3C=CC(=CC3)NC=4N=CC=5C=C(C(=O)N(C)C)N(C5N4)C6CCCC6)N7CCOCC7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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