Abemaciclib highly selective inhibits the complexes CDK4/ cyclin D1 (IC50 =2 nmol/L) and CDK6/cyclin D1 (IC50 =10 nmol/L), with no activity against other CDK/cyclin complexes or cell-cycle-related kinases within the nanomolar ranges, except for inhibition of CDK9 at IC50 at least five times higher. Besides the cell-cycle dependent activity, abemaciclib is able to boost antitumor immunity by potentiating tumor antigen presentation and selectively suppressing proliferation of regulatory T (Treg) cells at the same time. Consistent with its activity against CDK4 and CDK6, abemaciclib inhibits RB phosphorylation and leads to G1 arrest in RB-proficient cell lines. In vitro, treatment with abemaciclib resulted in increased activation of human T cells and upregulated expression of antigen presentation genes in MCF-7 breast cancer cells.
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Abemaciclib
Dangerous GoodsCAS number：1231929-97-7 molecular formula：C27H32F2N8
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | L01XE50 | 5-(4-ethylpiperazin-1-ylmethyl)pyridin-2-yl)-(5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-3H-benzimidazol-5-yl)pyrimidin-2-yl)amine | EX-A521 | LY 2835219 (free base) | NSC783671 | NSC-783671 | 5-(4-ethylpiperazin-1-ylmethyl)pyridin-2-yl)-(5-fluor | ||
| CAS number | 1231929-97-7 | molecular formula | C27H32F2N8 |
| molecular weight | 506.59 g/mol | Exact mass | - |
| PSA | 75.000 Ų | logp | 3.8 |
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Safety information
pictogram：
GHS08
Signal word：
Danger
Hazard Statement：
H373: 通过长时间或反复暴露对器官造成损害 H410: 对水生生物有剧毒并具有长期持续影响 H360: 可能损害生育力或未出生的孩子
Statement of Preventive Measures：
P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P308+P313: 如接触到或有疑虑：求医/就诊。 P314: 如果你感到不适，请就医。
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