abemaciclib mesylate (LY2835219)

Catalog No.S7158

abemaciclib mesylate (LY2835219) Chemical Structure

Molecular Weight(MW): 602.7

abemaciclib (LY2835219) is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.

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Cited by 19 Publications

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Choose Selective CDK Inhibitors

Biological Activity

Description abemaciclib (LY2835219) is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.
Targets
CDK4 [1]
(Cell-free assay)		 CDK6 [1]
(Cell-free assay)
2 nM 10 nM
In vitro

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. 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. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells  MmfXSpVv[3Srb36gZZN{[Xl? NXjhPXM2PTBibXnudy=> MXPDc41x\XSrdHn2[UBqdmirYnn0bY9vKG:oIHj1cYFvKEOGS{SvZ5lkdGmwIFSxJIV5eHKnc4Pl[EBqdiCrboPlZ5Qh[2WubIOgZZN{\XO|ZXSgZZMheGixc4Doc5J6dGG2aX;uJI9nKEOWUl[gZYZ1\XJiNUCgcYlveyCkeTDNbYNp[WWuaYOtUYVvfGWwIIDsc5Qh[W6jbInzbZMhcW5icILld4Vv[2Vib3[gRXRRNCCNaU2wMlYhdk1? MnfaNlYyOTV3N{G=
insect cells  NYjvb25CTnWwY4Tpc44h[XO|YYm= MVG1NEBucW6| M4HPe2lvcGmkaYTpc44hd2ZiaIXtZY4hS0SNND;jfYNtcW5iREGg[ZhxemW|c3XkJIlvKGmwc3XjeEBk\WyuczDhd5Nme3OnZDDhd{BxcG:|cHjvdplt[XSrb36gc4YhS1SURjDh[pRmeiB3MDDtbY5{KGK7IH3pZ5JweGyjdHWgd4NqdnSrbHzheIlwdiClb4XueIVzNCCLQ{WwQVIhdk1? MkP1NlYyOTV3N{G=
human COLO205 cells NHHXcIdHfW6ldHnvckBie3OjeR?= M1jlNlI1KGh? NWXSd|ZVUW6qaXLpeIlwdiCxZjDDSGs1NzZiaX6gbJVu[W5iQ1;MU|IxPSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHJjKHCqb4PwbI9zgWyjdHnvckBi\nSncjCyOEBpenNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCuYYPldk1{[2Gwbnnu[{BndHWxcnXzZ4Vv[2VibXnjdo9xdGG2ZTDjfZRwdWW2cnnjJIFv[Wy7c3nz NE\DZ2YzPjFzNUW3NS=>
human COLO205 cells Mn7BSpVv[3Srb36gZZN{[Xl? MXGyOEBp NVHi[m9qUW6qaXLpeIlwdiCxZjDDSGs1NzZiaX6gbJVu[W5iQ1;MU|IxPSClZXzsd{Bie3Onc4Pl[EBieyCvYYjpcZVuKGOnbHygZ5lkdGViYYLy[ZN1KGG2IFexJJBp[XOnIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtd3diY4n0c41mfHKrYzDhcoFtgXOrcx?= MWmyOlEyPTV5MR?=

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Assay
Methods Test Index PMID
Western blot
p-Rb(S780) / Rb / p21; 

PubMed: 26909611     


Effects of LY2835219 on RB phosphorylation and p21 expression were evaluated by immunoblotting at indicated concentrations (A)

p-ERK / ERK / p-Akt / Akt / p-mTOR(S2448) / mTOR; 

PubMed: 26909611     


Effects of LY2835219 on RB phosphorylation and p21 expression were evaluated by immunoblotting at indicated time points (B).

pRb(S795) / E2F1 / Cyclin A2 / Cyclin E2; 

PubMed: 27748766     


(c) MCF-7 and MR cells were treated with 100 nm LY2835219 and collected at indicated times. Immunoblots were performed with the indicated antibodies. (d) MCF-7 and MR cells were treated with increasing concentrations of LY2835219 and harvested after 24 h; lysates were then subjected to immunoblotting.

26909611 27748766
Growth inhibition assay
Cell viability; 

PubMed: 26909611     


Cell viability of OSC-19, FaDu, and YD-10B cells treated with LY2835219 at indicated concentrations. Data are representative of three independent experiments: mean ± SEM.

26909611
In vivo LY2835219 saturates BBB efflux with an unbound plasma IC50 of about 95 nM. The percent of dose in brain for LY2835219-MsOH is 0.5–3.9%. In both a subcutaneous and intracranial human glioblastoma model (U87MG), LY2835219-MsOH suppressed tumor growth in a dose-dependent manner both as a single agent, and in combination with temozolomide. [1]

Protocol

Solubility (25°C)

In vitro Water 100 mg/mL (165.92 mM)
DMSO 83 mg/mL (137.71 mM)
Ethanol 24 mg/mL (39.82 mM)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
water
For best results, use promptly after mixing. 		100mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 602.7
Formula

C27H32F2N8.CH4O3S
CAS No. 1231930-82-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02327143 Completed Drug: LY2835219|Drug: ¹³C₈-LY2835219 Healthy Volunteers Eli Lilly and Company January 2015 Phase 1
NCT02256267 Completed Drug: LY2835219|Drug: Rifampin Healthy Volunteers Eli Lilly and Company October 2014 Phase 1
NCT02059148 Completed Drug: LY2835219 Healthy Volunteers Eli Lilly and Company February 2014 Phase 1
NCT02014129 Completed Drug: LY2835219 Neoplasm Metastasis|Lymphoma Eli Lilly and Company December 18 2013 Phase 1
NCT01913314 Completed Drug: [^14C]-LY2835219 Healthy Volunteers Eli Lilly and Company August 2013 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Is your product S7158 LY2835219 “mesylate salt form”?

  • Answer:

    Our S7158 LY2835219 is mesylate salt form.

selleck catalog

CDK Signaling Pathway Map

CDK Inhibitors with Unique Features

  • Selective CDK Inhibitors

    BS-181 HCl : CDK7-selective, IC50=21 nM.

  • Selective CDK Inhibitors

    SNS-032 (BMS-387032) : CDK2-selective, IC50=48 nM.

  • CDK Inhibitor in Clinical Trial

    Palbociclib (PD0332991) Isethionate : Phase III for Metastatic Breast Cancer.

  • Newest CDK Inhibitor

    NU6027 : Potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.

  • Classic CDK Inhibitor

    Palbociclib (PD-0332991) HCl : Highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 2/3.

Related CDK Products

  • SU9516 New

    SU 9516 is a 3-substituted indolinone CDK inhibitor with IC50 of 22 nM, 40 nM, and 200 nM for CDK2, CDK1, and CDK4, respectively.

  • Ro-3306 New

    RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases.

  • Purvalanol A New

    Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively.

  • Palbociclib (PD-0332991) HCl

    Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

    Features:Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).

  • Palbociclib (PD0332991) Isethionate

    Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

    Features:The 1st specific inhibitor for CDK4/6 to show promise in multiple cancers.

  • Dinaciclib (SCH727965)

    Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Phase 3.

  • Flavopiridol HCl

    Flavopiridol HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.

  • Roscovitine (Seliciclib,CYC202)

    Roscovitine (Seliciclib, CYC202) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM in cell-free assays. It shows little effect on CDK4/6. Phase 2.

  • Ribociclib (LEE011)

    Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.

  • SNS-032 (BMS-387032)

    SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. Phase 1.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID