research use only
Cat.No.S5188
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In vitro |
DMSO
: 13 mg/mL
(23.52 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Molecular Weight | 552.63 | Formula | C27H36N8O5 |
Storage (From the date of receipt) | 3 years -20°C powder |
|---|---|---|---|---|---|
| CAS No. | 1374639-75-4 | -- | Storage of Stock Solutions |
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| Synonyms | LEE011 succinate | SMILES | CN(C)C(=O)C1=CC2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2[N]1C5CCCC5.OC(=O)CCC(O)=O | ||
Read more about storage stability stock solution CAS number SMILES
| Targets/IC50/Ki |
CDK4
(Cell-free assay) 10 nM
CDK6
(Cell-free assay) 39 nM
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|---|---|
| In vitro |
LEE011, as dual CDK4/CDK6 inhibitor, significantly inhibits the growth of 12 of 17 neuroblastoma cell lines with mean IC50 of 307 nM. The growth inhibition of neuroblastoma cell lines is primarily cytostatic and is mediated by a G1 cell-cycle arrest and cellular senescence. |
| In vivo |
LEE011 (200 mg/kg daily, p.o.) significantly causes tumor growth delay in mice harboring the BE2C or 1643 xenografts with no weight loss or other signs of toxicity. |
References |
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(data from https://clinicaltrials.gov, updated on 2026-05-26)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT07237256 | RECRUITING | Breast Cancer |
UNICANCER |
2025-12-18 | PHASE3 |
| NCT06849947 | NOT_YET_RECRUITING | Breast Cancer Metastatic |
Yeon Hee Park |
2026-02-01 | PHASE2 |
| NCT02813135 | RECRUITING | Pediatric Cancer |
Gustave Roussy, Cancer Campus, Grand Paris |
2016-08-03 | PHASE1; PHASE2 |
| NCT07423611 | NOT_YET_RECRUITING | Breast Cancer |
Fudan University |
2026-10-01 | PHASE2 |
| NCT03424005 | RECRUITING | Metastatic Breast Cancer |
Hoffmann-La Roche |
2018-03-30 | PHASE1; PHASE2 |
| NCT06953882 | RECRUITING | HER2 Negative Breast Cancer |
Yale University |
2025-07-09 | PHASE2 |
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