1231929-97-7 Usage
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1231929-97-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,3,1,9,2 and 9 respectively; the second part has 2 digits, 9 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1231929-97:
(9*1)+(8*2)+(7*3)+(6*1)+(5*9)+(4*2)+(3*9)+(2*9)+(1*7)=157
157 % 10 = 7
So 1231929-97-7 is a valid CAS Registry Number.
1231929-97-7Relevant articles and documents
A synthesis of abemaciclib utilizing a Leuckart-Wallach reaction
Frederick, Michael O.,Kjell, Douglas P.
, p. 949 - 951 (2015)
A concise total synthesis of CDK 4/6 inhibitor abemaciclib is described. The synthesis uses a Suzuki coupling, followed by a Hartwig-Buchwald amination to join three of the four subunits. The final step is a reductive amination utilizing Leuckart-Wallach conditions. Key to the Leuckart-Wallach reaction was the addition of trimethyl orthoformate to remove water formed during the reaction, allowing the reaction to go to completion.
Abecheli intermediate and simple preparation method of Abemaciclib
-
, (2019/10/01)
The invention relates to an Abemaciclib intermediate and a simple preparation method of Abemaciclib. The Abemaciclib intermediate is 1-isopropyl-2-methyl-4-fluorine-6-(3-dimethylamino-2-fluorine) acryloyl-1H-benzimidazole (V), and also provides a preparation method of the Abemaciclib intermediate. The Abecheli intermediate and 5-(4-ethylpiperazine-1-yl) methyl-2-pyridylguanidine are subjected to pyrimidine cyclization reaction to prepare Abemaciclib (I). The method has the advantages of cheap and easily available raw materials, good stability of raw materials and intermediate products, mild reaction conditions, high reaction selectivity, high atom economy in the reaction process, high product purity and yield, low cost, less three wastes, environmental protection and contribution to the industrial production of Abemaciclib.
ABEMACICLIB FORM IV
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Page/Page column 13; 14, (2017/07/14)
The present invention relates to a crystalline form of abemaciclib, a method of preparing the same, as well as a pharmaceutical composition comprising the same.