Name | Abemaciclib |
Synonyms | Abemaciclib LY 2835219 (free base) Abemaciclib (LY2835219) Bemaciclib(LY2835219, abemaciclib) |
CAS | 1231929-97-7 |
Molecular Formula | C27H32F2N8 |
Molar Mass | 506.5934 |
Density | 1.32±0.1 g/cm3(Predicted) |
Boling Point | 689.3±65.0 °C(Predicted) |
Solubility | 10 mM in DMSO |
pKa | 7.69±0.10(Predicted) |
Storage Condition | -20℃ |
Physical and Chemical Properties | Bioactive Abemaciclib (LY2835219) is a cell cycle inhibitor selective for CDK4/6. The IC50 values in cell-free tests are 2 nM and 10 nM respectively. |
Use | Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor, which can inhibit the activity of CDK4/CDK6 with IC50 of 2 nM and 10 nM respectively. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.974 ml | 9.87 ml | 19.74 ml |
5 mM | 0.395 ml | 1.974 ml | 3.948 ml |
10 mM | 0.197 ml | 0.987 ml | 1.974 ml |
5 mM | 0.039 ml | 0.197 ml | 0.395 ml |
Introduction
Abexilib is an oral cyclin-dependent kinase CDK4/6 inhibitor. In HR, HER2-breast cancer cells, CDK4 and CDK6 promote the phosphorylation of retinoblastoma protein (retinoblastoma protein,Rb), and promote cell cycle progress and cell proliferation. Abemaciclib can inhibit the phosphorylation of Rb and block the progress of cells from G1 phase to S phase of cell cycle, thus leading to cell aging and apoptosis.
new drug for breast cancer
On December 29, 2020, Eli Lilly announced that its new anti-tumor drug Weixuan® (Abexili Tablets) was approved by the National Drug Administration (NMPA) for hormone receptor positive (HR) and human epidermal growth factor receptor 2 negative (HER2-) Locally advanced or metastatic breast cancer:(1) Combined use with aromatase inhibitors as the initial endocrine therapy for postmenopausal female patients. (2) Combined with fulvestrant for patients with disease progression after previous endocrine therapy. As a result, abesilli (Abemaciclib) became the second CDK4/6 inhibitor listed in China after palbocilli.
Indications
Abexilib in combination with flovesetron (fulvestrant) for the treatment of adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer. Verzenio used alone to treat the same group of patients who have received endocrine therapy and chemotherapy but have metastatic cancer.