Identification | Back Directory | [Name]
Abemaciclib | [CAS]
1231929-97-7 | [Synonyms]
CS-814 abecilee Abemaciclib Abemaciclib D7 Abemaciclib D10 ABEMACICLIB BASE Abemaciclib, >=98% Abemaciclib Powder Abemaciclib free base CDK4/6 dual inhibitor LY2835219 (free base) LY-2835219 (free base) LY 2835219 (free base) LY2835219(Abemaciclib) Abemaciclib (LY2835219) Bemaciclib(LY2835219free base LY2835219free base,Abemaciclib abemaciclib(CDK 4/6 inhibitor) Abemaciclib Mesylate (Verzenio) Bemaciclib(LY2835219, abemaciclib) ethyl-1-(propan-2-yl)-1H-benzimidazol-6-yl]pyrimidin-2-amine inhibit,LY-2835219,LY 2835219,Abemaciclib,Inhibitor,Cyclin dependent kinase,CDK LY2835219;LY-2835219;LY 2835219;ABEMACICLIB;CDK4/6 DUAL INHIBITOR;LY-2835219 FREE BASE N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine 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 N-{5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl}-5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-1,3-benzodiazol-5-yl)pyrimidin-2-amine N-(5-((4-Ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine 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 2-Pyrimidinamine,N-[5-[(4-ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]- | [Molecular Formula]
C27H32F2N8 | [MDL Number]
MFCD22665744 | [MOL File]
1231929-97-7.mol | [Molecular Weight]
506.59 |
Chemical Properties | Back Directory | [Boiling point ]
689.3±65.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [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) |
Hazard Information | Back Directory | [Uses]
Abemaciclib is a potent and selective inhibitor of cyclin-dependent kinases, CDK4 and CDK6, as a method to inhibit the proliferation of cancer cells. | [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. |
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