LY2835219(Abemaciclib)

  Cat. No.:  DC5062   Featured
Chemical Structure
1231930-82-7
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Cas No.: 1231930-82-7
Chemical Name: Abemaciclib mesylate
Synonyms: 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;abemaciclib (LY2835219);Bemaciclib;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-methylethyl)-1H-benzimidazol-6-yl]...;N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyr;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;6 dual inhibitor;ABEMACICLIB;CDK4;CS-1229;LY-2835219;QCR-274;Bemaciclib(salt);Abemaciclib methanesulfonate
SMILES: CC(N1C2=CC(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)=CC(F)=C2N=C1C)C.CS(=O)(O)=O
Formula: C28N8O3F2SH36
M.Wt: 602.699
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Abemaciclib (LY2835219) (methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively.
In Vivo: Abemaciclib (LY2835219) (45 mg/kg, p.o.) in combination with everolimus 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].
In Vitro: Abemaciclib (LY2835219) reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells[1]. Abemaciclib (LY2835219) shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; Abemaciclib inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC50 values of 395, 260, and 463 nM, respectively[2]. Abemaciclib (LY2835219) inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells[3].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC27001 SR-4835 SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13.
DC70595 MFH290 MFH290 (MFH-290) is a potent, highly selective, covalent inhibitor of CDK12/13 with IC50 of 25/49 nM.MFH290 forms a covalent bond with Cys-1039 of CDK12, and CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290.MFH290 exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes.MFH290 restored Pol II CTD phosphorylation and DNA damage repair gene expression AND augments the antiproliferative effect of the PARP inhibitor olaparib.
DC50184 dCeMM3 dCeMM3 (Compound 3) is a glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex.
DC49082 CDK5-IN-2 CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor with IC50s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively.
DC44518 CDK7-IN-3 CDK7-IN-3 is a selective CDK7 inhibitor with a KD of 0.059 nM. CDK7-IN-3 shows poor inhibition on CDK2 (Ki=390 nM), CDK9 (Ki=290 nM), CDK12 (Ki=78 nM). CDK7-IN-3 induce apoptosis in tumor cells and has antitumor activity.
DC28661 Cdc7-IN-7 Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
DC28660 Cdc7-IN-6 Cdc7-IN-6 (compound I-D) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity.
DC28659 Cdc7-IN-5 Cdc7-IN-5 (compound I-B) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
DC7493 SB1317(TG-02) SB1317(TG-02) is a novel small molecule potent CDK2/JAK2/FLT3 inhibitor with IC50s of 13/73/56 nM respectively.
DC11282 THZ2 THZ2 is a potent and selective CDK7 inhibitor with IC50 of 13.9 nM.
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