LY2835219 Chemical Structure

LY2835219 Chemical Structure
Molecular Weight: 602.7

Validation & Quality Control

Customer Product Validation(1)

Quality Control & MSDS

CDK Inhibitors with Unique Features

  • Selective CDK Inhibitors

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

Product Information

  • Compare CDK Inhibitors
    Compare CDK Products
  • Research Area

Product Description

Biological Activity

Description 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)
IC50 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]
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]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Sanchez-Martinez et al. Mol Cancer Ther, 2011,10(11 Suppl), Abstract nr B234.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02327143 Completed Healthy Volunteers Eli Lilly and Company January 2015 Phase 1
NCT02256267 Completed Healthy Volunteers Eli Lilly and Company October 2014 Phase 1
NCT02117648 Completed Neoplasm|Neoplasm Metastasis Eli Lilly and Company April 2014 Phase 1
NCT02057133 Active, not recruiting Breast Neoplasms Eli Lilly and Company March 2014 Phase 1
NCT02059148 Completed Healthy Volunteers Eli Lilly and Company February 2014 Phase 1

view more

Chemical Information

Download LY2835219 SDF
Molecular Weight (MW) 602.7
Formula

C27H32F2N8.CH4O3S

CAS No. 1231930-82-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 83 mg/mL (137.71 mM)
Water 100 mg/mL (165.92 mM)
Ethanol 24 mg/mL (39.82 mM)
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 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)

Customer Product Validation (1)


Click to enlarge
Rating
Source Biochem J 2014 459(3), 513-24. LY2835219 purchased from Selleck
Method Western blot
Cell Lines HT29 cells
Concentrations 0.3 uM
Incubation Time 48 h
Results CDK4/6 selective inhibitor, LY2835219, and to a lesser extent serum withdrawal, induced BIK expression in HT29 cells.

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.

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

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related CDK Products

  • SU9516

    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

    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

    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 (Alvocidib) 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.

Recently Viewed Items

Tags: buy LY2835219 | LY2835219 supplier | purchase LY2835219 | LY2835219 cost | LY2835219 manufacturer | order LY2835219 | LY2835219 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us