Other grades of this product :
| Abemaciclib Basic information |
| Abemaciclib Chemical Properties |
| Boiling point | 689.3±65.0 °C(Predicted) | | density | 1.32±0.1 g/cm3(Predicted) | | solubility | insoluble in H2O; ≥4.83 mg/mL in DMSO with gentle warming and ultrasonic; ≥6.34 mg/mL in EtOH with gentle warming | | form | solid | | pka | 7.69±0.10(Predicted) |
| Abemaciclib Usage And Synthesis |
| Biological Activity | ly2835219 is an orally available cyclin-dependent kinase (cdk) inhibitor that targets the cdk4 (cyclin d1) and cdk6 (cyclin d3) cell cycle pathway, with potential antineoplastic activity. cdk4/6 dual inhibitor ly2835219 specifically inhibits cdk4 and 6, thereby inhibiting retinoblastoma (rb) protein phosphorylation in early g1. inhibition of rb phosphorylation prevents cdk-mediated g1-s phase transition, thereby arresting the cell cycle in the g1 phase, suppressing dna synthesis and inhibiting cancer cell growth. overexpression of the serine/threonine kinases cdk4/6, as seen in certain types of cancer, causes cell cycle deregulation. | | Enzyme inhibitor | This oral cell cycle inhibitor (FWfree-base = 506.61 g/mol; FWmesylate-salt =
602.70 g/mol; CAS 1231930-82-7 (mesylate salt) ), also known as
LY2835219 and N-[5-[ (4-ethyl-1-piperazinyl) methyl]-2-pyridinyl]-5-
fluoro-4-[4-fluoro-2-methyl-1- (1-methylethyl) -1H-benzimidazol-6-yl]-2-
pyrimidinamine, targets the cyclin-dependent kinase CDK4, or cyclin D1
(IC50 = 2 nM) and CDK6, or cyclin D3 (IC50 = 6 nM), inhibiting
retinoblastoma (Rb) protein phosphorylation in early G1, thereby arresting
the cell cycle in the G1, suppressing DNA synthesis, and inhibiting cancer
cell growth. LY2835219 inhibits activation of AKT and ERK, but not
mTOR. |
| Abemaciclib Preparation Products And Raw materials |
| Raw materials | EthaniMidaMide, N-(4-broMo-2,6-difluorophenyl)-N'-(1-Methylethyl)--->4-Bromo-2,6-difluoroaniline-->2-Bromopyridine-5-carbaldehyde-->Piperazine, 1-[(6-broMo-3-pyridinyl)Methyl]-4-ethyl--->N-Isopropylacetamide-->1H-BenziMidazole, 6-(2-chloro-5-fluoro-4-pyriMidinyl)-4-fluoro-2-Methyl-1-(1-Methylethyl)--->1H-BenziMidazole, 4-fluoro-2-Methyl-1-(1-Methylethyl)-6-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)--->4-AMINO-3,5-DIFLUOROACETOPHENONE-->5-((4-Ethylpiperazin-1-yl)methyl)pyridin-2-amine-->6-Bromo-4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-->1-Ethylpiperazine-->2,6-Difluoroaniline |
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