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LY2835219

LY2835219 structure

CAS No:
1231930-82-7
Formula:
C28H36F2N8O3S
Chemical Name:
LY2835219
Synonyms:
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]-, methanesulfonate (1:1);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 methanesulfonate (1:1)LY2835219;LY2835219 mesylate;Bemaciclib(salt);Bemaciclib;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,methanesulfonic acid;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 methanesulfonate;N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methyle
Categories:
Biochemical Engineering > Inhibitors

Description

Abemaciclib (LY2835219) (methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively.

Abemaciclib Mesylate is the mesylate salt of abemaciclib, an orally available cyclin-dependent kinase (CDK) inhibitor that targets the cyclin D1-CDK4 and cyclin D3-CDK6 cell cycle pathway, with potential antineoplastic activity. Abemaciclib 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.

LY2835219 Basic Attributes

Molecular Weight：

602.6990464

Exact Mass：

602.259888

UNII：

KKT462Q807

DSSTox ID：

DTXSID90856159

NCI Thesaurus Code：

C162507

Characteristics

PSA：

138

XLogP3：

5.47050

Drug Information

MeSH Entry Terms：

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

LY2835219 Use and Manufacturing

LY2835219 is an orally-bioavailable dual inhibitor of cyclin-dependent kinase 4 (CDK4) and CDK6 (IC50s = 2 and 10 nM, respectively). Through this mechanism, it blocks phosphorylation of retinoblastoma protein, resulting in arrest of cell cycling in the G1 phase. LY2835219 has antitumor action against xenografts when used alone or in combination with other chemotherapeutic compounds.[Cayman Chemical]

Computed Properties

Molecular Weight:602.7
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:12
Rotatable Bond Count:7
Exact Mass:602.25991454
Monoisotopic Mass:602.25991454
Topological Polar Surface Area:138
Heavy Atom Count:42
Complexity:815
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

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HANGZHOU LEAP CHEM CO., LTD. Contact Supplier

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LY2835219 mesylate

CAS No.: 1231930-82-7

Grade: industrial Grade

Content: 98%

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