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2017年1月14日星期六

EOS Med Chem produce Abemaciclib ( LY2835219) 1231929-97-7 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Name: Abemaciclib ( LY2835219)
CAS#: 1231929-97-7 (free base)
Chemical Formula: C27H32F2N8
Exact Mass: 506.2718
Molecular Weight: 506.59339
Elemental Analysis: C, 64.01; H, 6.37; F, 7.50; N, 22.12

EOS Med Chem produce Abemaciclib ( LY2835219) 1231929-97-7  in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Abemaciclib ( LY2835219) 1231929-97-7  Intermediates, EOS Med Chem have 8; Abemaciclib ( LY2835219) 1231929-97-7  Impurity we have 10, all from GMP, FDA plaAnt.
Now Abemaciclib ( LY2835219) 1231929-97-7  DMF document is preparing.
Until 2016, Aug, Abemaciclib ( LY2835219) 1231929-97-7  more than produced 25kg API, 120kg Intermediates

Related CAS#
CAS#1231929-97-7 (LY2835219 free base)
CAS# 1231930-82-7 (LY2835219 mesylate salt).

Abemaciclib ( LY2835219) 1231929-97-7 Abemaciclib ( LY2835219)
Abemaciclib ( LY2835219) Intermediate 67567-26-4, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Abemaciclib ( LY2835220) Intermediate 1180132-17-5, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Abemaciclib ( LY2835221) Intermediate 1231930-42-9, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Abemaciclib ( LY2835222) Intermediate 1231929-97-7, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Abemaciclib ( LY2835223) Intermediate 1231930-33-8, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Abemaciclib ( LY2835224) Intermediate 1231930-82-7, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.



Description: Abemaciclib, also known as LY2835219, is orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. LY2835219 inhibits CDK4 and CDK6 with low nanomolar potency. 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.
Synonym: LY2835219; LY2835219; LY 2835219; Abemaciclib.
IUPAC/Chemical Name: 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
SMILES Code: CC1=NC2=C(F)C=C(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)C=C2N1C(C)C

1: Yadav V, Burke TF, Huber L, Van Horn RD, Zhang Y, Buchanan SG, Chan EM, Starling JJ, Beckmann RP, Peng SB. The CDK4/6 Inhibitor LY2835219 Overcomes Vemurafenib Resistance Resulting from MAPK Reactivation and Cyclin D1 Upregulation. Mol Cancer Ther. 2014 Aug 13. pii: molcanther.0257.2014. [Epub ahead of print] PubMed PMID: 25122067.
2: Gelbert LM, Cai S, Lin X, Sanchez-Martinez C, Del Prado M, Lallena MJ, Torres R, Ajamie RT, Wishart GN, Flack RS, Neubauer BL, Young J, Chan EM, Iversen P, Cronier D, Kreklau E, de Dios A. 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. 2014 Jun 13. [Epub ahead of print] PubMed PMID: 24919854.
3: Tate SC, Cai S, Ajamie RT, Burke T, Beckmann RP, Chan EM, De Dios A, Wishart GN, Gelbert LM, Cronier DM. Semi-mechanistic pharmacokinetic/pharmacodynamic modeling of the antitumor activity of LY2835219, a new cyclin-dependent kinase 4/6 inhibitor, in mice bearing human tumor xenografts. Clin Cancer Res. 2014 Jul 15;20(14):3763-74. doi: 10.1158/1078-0432.CCR-13-2846. Epub 2014 May 21. PubMed PMID: 24850847.
4: Dickson MA. Molecular pathways: CDK4 inhibitors for cancer therapy. Clin Cancer Res. 2014 Jul 1;20(13):3379-83. doi: 10.1158/1078-0432.CCR-13-1551. Epub 2014 May 2. PubMed PMID: 24795392.