Mechanism of action Current clinical trials Study in vivo References
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Abemaciclib mesylate (LY2835219)

Mechanism of action Current clinical trials Study in vivo References
Abemaciclib mesylate (LY2835219) Structure
Abemaciclib mesylate (LY2835219)
  • CAS No.1231930-82-7
  • Chemical Name:Abemaciclib mesylate (LY2835219)
  • CBNumber:CB02628066
  • Molecular Formula:C28H36F2N8O3S
  • Formula Weight:602.71
  • MOL File:1231930-82-7.mol
Abemaciclib mesylate (LY2835219) Property
  • storage temp. -20°
  • solubility Soluble in DMSO (up to at least 25 mg/ml) or in Water (up to at least 25 mg/ml).
  • form solid
  • color Off-white
  • Stability Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month.
  • CAS DataBase Reference 1231930-82-7
  • FDA UNII KKT462Q807
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H315-H319-H335
  • Precautionary statements P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501

Abemaciclib mesylate (LY2835219) Chemical Properties,Usage,Production

  • Mechanism of action Many human tumors acquire alterations, which can lead to the activation of cyclin-dependent kinases (CDKs)—CDK4 and CDK6. These alterations include mutations that directly activate CDK4 and CDK6, gene amplifications, which increase expression of various protein activators such as cyclin D, as well as genetic losses, which reduce expression of protein inhibitors such as p16.
    Abemaciclib(previously known as 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.
  • Current clinical trials Abemaciclib(LY2835219) is being investigated in clinical trials in patients with breast cancer, non-small cell lung cancer, and pancreatic cancer, including a combination clinical trial in immuno-oncology.
    As of early 2016 Abemaciclib is involved in 3 Phase III clinical trials:
    The JUNIPER Study is comparing Abemaciclib against Erlotinib in patients with stage IV Non-small-cell lung carcinoma.
    The MONARCH 2 study is investigating the effectiveness of Abemaciclib in combination with Fulvestrant for women with breast cancer. It is due to end in Feb 2017.
    The MONARCH 3 study is investigating the effectiveness of Abemaciclib, plus either anastrozole or letrozole, as a first-line treatment for women with breast cancer. The trail is expected to end in June 2017.
  • Study in vivo The dose percentage of LY2835219-MsOH treating brain was 0.5-3.9%. LY2835219-MsOH could treat subcutaneous and intracranial glioma models (U87MG), inhibiting tumor growth, and the effect is dose-dependent, whether alone or in combination with mozolomide.
  • References http://www.lillyoncologypipeline.com/molecule/cdk-4-and-cdk-6-inhibitor/overview
    https://en.wikipedia.org/wiki/Abemaciclib
    https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=706364
  • Description Abemaciclib (1231930-82-7) is a potent and selective CDK4/6 inhibitor (IC50?= 2 nM and 10 nM respectively).1?It caused G1 cell cycle arrest in colo-205 colorectal cells, MDA-MB-361 breast cancer cells, and MV4-11 AML cells. Abemaciclib was also active in several human tumor xenograft models. It displayed efficacy in patients with various solid tumors including breast cancer, non-small cell lung cancer. Glioblastoma, melanoma, colorectal cancer, and hormone receptor-positive breast cancer.2?Abemaciclib induced a T cell inflamed tumor microenvironment and enhanced the efficacy of PD-L1 checkpoint blockade in MCF-7 breast cancer cells.3?FDA approved for the treatment of advanced breast cancers.
  • Uses 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 is an CDK4/6 protein kinase inhibitor with potential antitumor effects.
  • Uses 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]
  • in vivo

    Abemaciclib (LY2835219) (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor[1].
    Abemaciclib (LY2835219) (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model[2].

  • 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.
  • IC 50 Cdk4/cyclin D1: 2 nM (IC50); CDK6/cyclinD1: 10 nM (IC50); CDK9/cyclinT1: 57 nM (IC50); CDK5/p35: 287 nM (IC50); Cdk5/p25: 355 nM (IC50); CDK2/cyclinE: 504 nM (IC50); CDK1/cyclinB1: 1627 nM (IC50); CDK7/Mat1/cyclinH1: 3910 nM (IC50); PIM1: 50 nM (IC50); PIM2: 3400 nM (IC50); HIPK2: 31 nM (IC50); DYRK2: 61 nM (IC50); CK2: 117 nM (IC50); GSK3b: 192 nM (IC50); JNK3: 389 nM (IC50); FLT3 (D835Y): 403 nM (IC50); DRAK1: 659 nM (IC50); FLT3: 3960 nM (IC50)
  • References 1) Gelbert?et al.?(2014),?Preclinical characterization of the CDK4/6 inhibitor LY2835219: In-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine; Invest. New Drugs,?32?825 2) Patnail?et al.?(2016),?Efficacy and Safety of Abemaciclib, an Inhibitor of CDK4 and CDK6, for Patients with Breast Cancer, Non-small Cell Lung Cancer, and Other Solid Tumors; Cancer Discov.,?6?740 3) Schaer?et al. (2018),?The CDK4/6 Inhibitor Abemaciclib Induces a T Cell Inflamed Tumor Microenvironment and Enhances the Efficacy of PD-L1 Checkpoint Blockade; Cell Rep.,?22?2978
Abemaciclib mesylate (LY2835219) Preparation Products And Raw materials
Raw materials
Preparation Products
Abemaciclib mesylate (LY2835219) Suppliers
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Abemaciclib mesylate (LY2835219) Spectrum
1231930-82-7, Abemaciclib mesylate (LY2835219)Related Search:
  • Inhibitors
  • 抑制剂
  • 杂质对照品
  • 药靶配体
  • 对照品
  • 细胞生物学试剂
  • 小分子抑制剂，天然产物
  • 细胞周期
  • CH4O3SC27H32F2N8
  • C27H32F2N8CH4O3S
  • C28H36F2N8O3S
  • 化合物ABEMACICLIB MESYLATE,10 MM DMSO 溶液
  • ABEMACICLIB METHANESULFONATE(阿贝西利)
  • 化合物 ABEMACICLIB MESYLATE
  • 甲磺酸阿贝西利
  • N-[5-[(4-乙基-1-哌嗪基)甲基]-2-吡啶基]-5-氟-4-[4-氟-2-甲基-1-(1-甲基乙基)-1H-苯并咪唑- 6-基]-2-嘧啶胺甲磺酸盐
  • 甲磺酸LY2835219
  • N-[5-[(4-乙基-1-哌嗪基)甲基]-2-吡啶基]-5-氟-4-[4-氟-2-甲基-1-(1-甲基乙基)-1H-苯并咪唑-6-基]-2-嘧啶胺甲烷磺酸酯
  • 阿贝西利甲磺酸
  • 阿贝昔利布甲磺酸盐
  • 玻马西林甲磺酸盐
  • LY2835219盐
  • CDK4/6抑制剂(LY2835219)
  • 阿贝西利甲磺酸盐
  • N-[5-[(4-乙基-1-哌嗪基)甲基]-2-吡啶基]-5-氟-4-[4-氟-2-甲基-1-(1-甲基乙基)-1H-苯并咪
  • LY 2835219N-[5-[(4-乙基-1-哌嗪基)甲基]-2-吡啶基]-5-氟-4-[4-氟-2-甲基-1-异丙基-1H-苯并咪唑-6-基]-2-嘧啶胺甲烷磺酸盐
  • N-(5-((4-甲基哌嗪-1-基甲基)吡啶-2-基)-5氟-4-(4-氟-1-异丙基-2-甲基-1H-苯并[D]咪唑-6-基)嘧啶-2-胺甲磺酸盐
  • N-[5-[(4-乙基-1-哌嗪基)甲基]-2-吡啶基]-5-氟-4-[4-氟-2-甲基-1-异丙基-1H-苯并咪唑-6-基]-2-嘧啶胺甲烷磺酸盐
  • LY2835219甲磺酸盐
  • 1231930-82-7
  • 2-Pyrimidinamine, N-[5-[(4-ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimida
  • Abemaciclib methanesulfonate, 10 mM in DMSO
  • N-(5-((4-Ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzodimidazol-6-yl)pyrimidin-2-amine mesylate
  • Bemaciclib
  • Abemaciclib Mesylate
  • LY2835219 USP/EP/BP
  • Abemaciclib (LY2835219) mesylate
  • Bamaciclib Mesylate
  • LY2835219; LY-2835219; LY 2835219
  • CS-806
  • Abemaciclib mesylate(LY2835219 mesylate)
  • LY2835219 (Abemaciclib) mesylate
  • ABEMACICLIB METHANESULFONATE (LY2835219 METHANESULFONATE)
  • LY2835219methanesulfonic acid
  • 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)
  • 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
  • LY2835219/LY-2835219
  • LY2835219
  • N-(5-((4-Ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H
  • ABEMACICLIB LY2835219 100MG
  • ABEMACICLIB (LY2835219);LY2835219;LY 2835219;LY-2835219
  • LY2835219 (methanesulfonate)
  • Abemaciclib mesylate(LY2835219)
  • Abemaciclib (methanesulfonate)
  • LY2835219 Ms salt, Abemaciclib Ms salt
  • N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methyle
  • 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-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

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