1211441-98-3
LEE011
CAS: 1211441-98-3
Molecular Formula: C23H30N8O
1211441-98-3 - Names and Identifiers
1211441-98-3 - Physico-chemical Properties
| Molecular Formula | C23H30N8O |
| Molar Mass | 434.54 |
| Density | 1.39±0.1 g/cm3(Predicted) |
| Boling Point | 730.8±70.0 °C(Predicted) |
| Solubility | DMSO: ≥ 4.3 mg/mL; DMSO: < 8.4 mg/mL |
| Appearance | solid |
| Color | Off-white |
| pKa | 8.67±0.10(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| Physical and Chemical Properties | Properties LEE011(Ribociclib) was used in its tartrate form. It is a slightly hygroscopic yellow to brown crystalline powder, soluble in aqueous acids. |
| Use | Application LEE011 (ribociclib) is an inhibitor of the cyclin D1 / CDK4 and CDK6 for the treatment of certain types of breast cancer. It is also being studied as a treatment for other drug-resistant cancers. |
| In vitro study | LEE011, a dual CDK4/CDK6 inhibitor, was able to significantly inhibit the growth of 12 out of 17 neurocytomas with a mean IC50 value of 307 nM. The inhibition of neurocytoma is mainly to inhibit the growth of cells, which is regulated by G1 cell cycle arrest and cell senescence. |
| In vivo study | LEE011 (200 mg/kg daily, P. O.) caused a significant growth delay of BE2C or 1643 cells in mice without weight loss or other signs of toxicity. |
1211441-98-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.301 ml | 11.506 ml | 23.013 ml |
| 5 mM | 0.46 ml | 2.301 ml | 4.603 ml |
| 10 mM | 0.23 ml | 1.151 ml | 2.301 ml |
| 5 mM | 0.046 ml | 0.23 ml | 0.46 ml |
Last Update：2024-01-02 23:10:35
1211441-98-3 - Uses and methods of synthesis
mechanism of action
cyclin-dependent kinases (CDKs)4 and 6 are enzymes that have been shown to promote cell division and proliferation in normal and cancer cells. Many cancer cells show abnormalities that increase the activity of CDKs, leading to the inactivation of certain tumor suppressor genes. ribociclib has been shown to be synergistic when used in combination with other drugs, such as ALK or MEK inhibitors, thereby improving the response. Again, this may be a result of "cross-talk" between signal paths. Simply blocking one pathway in cancer tumorigenesis can sometimes lead to "tumor compensation," where tumors compensate for blocked signaling pathways by using other pathways to survive. By blocking several pathways at the same time, it is considered that the compensatory capacity of the tumor is poor and a greater anti-tumor response is generally observed. The use of ribosomes in combination with other drugs has been shown to reduce resistance to these drugs. In other words, the development of drug resistance in cancer can be mitigated by the addition of ribosomes in the treatment regimen.
side effects
The most common side effects of LEE011 in the study, lowering blood counts, were mainly neutropenia (in 75% of patients compared to 5% on placebo), and anemia (18% vs. 5%). Gastrointestinal disorders were also common, such as Nausea (52% vs. 29%) and Diarrhea (35% vs. 22%), and alopecia (33% vs. 16%). The drug also increases QT Time and liver enzymes (alanine aminotransferase, aspartate aminotransferase).
biological activity
Ribociclib (LEE011) is an orally active, highly specific inhibitor of CDK4 and CDK6 with IC50 values of 10 nM and 39 nM, respectively. Phase 3.
Target
Target Value
CDK4
(Cell-free assay) 10 nM
CDK6
(Cell-free assay) 39 nM
in vitro studies
LEE011, a dual CDK4/CDK6 inhibitor, was able to significantly inhibit the growth of 12 out of 17 neurocytomas with a mean IC50 value of 307 nM. The inhibition of neurocytoma is mainly to inhibit the growth of cells, which is regulated by G1 cell cycle arrest and cell senescence.
in vivo studies
LEE011 (200 mg/kg daily, p. O.) caused a significant growth delay of BE2C or 1643 cells in mice without weight loss or other signs of toxicity.
Last Update：2024-04-10 22:29:15
Supplier List
Spot supply
Product Name: LEE011 Visit Supplier Webpage Request for quotationCAS: 1211441-98-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: LEE011 Visit Supplier Webpage Request for quotationCAS: 1211441-98-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History