Home Cell Cycle CDK inhibitor LY2857785 For research use only.

LY2857785

LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9(IC50=0.011 μM) and also inhibits other transcription kinases CDK8(IC50=0.016 μM) and CDK7 (IC50=0.246 μM).

LY2857785 Chemical Structure

LY2857785 Chemical Structure

CAS: 1619903-54-6

Selleck's LY2857785 has been cited by 2 publications

Purity & Quality Control

Batch: S751101 Ethanol] 42 mg/mL] false] DMSO] 23 mg/mL] false] Water] Insoluble] false Purity: 98.97%
98.97

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Biological Activity

Description LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9(IC50=0.011 μM) and also inhibits other transcription kinases CDK8(IC50=0.016 μM) and CDK7 (IC50=0.246 μM).
Targets
CDK9 [1]
(Cell-free assay)		 CDK8 [1]
(Cell-free assay)		 CDK7 [1]
(Cell-free assay)
0.011 μM 0.016 μM 0.246 μM
In vitro
In vitro LY2857785 shows good selectivity against a panel of 114 protein kinases, with only 5 other protein kinases inhibited with potency (IC50) less than 0.1 μmol/L, and a total of 14 kinases less than 1 μmol/L. At the cellular level, LY2857785 inhibits CTD P-Ser2 and CTD P-Ser5 in U2OS cells at IC50s 0.089 and 0.042 μM. Although LY2857785 inhibits CDK4, CDK6, and CDK2 enzymatic activities, it does not induce G1-S cell-cycle arrest. It also has activity against CDK1 (Histone H1 P-T153 inhibition IC50 0.241 μmol/L). However LY2857785 only induces a moderate G2–M DNA content increase, from 35% to 55%, with EC50 0.135 μmol/L. LY2857785 inhibits hematologic and solid tumor cell proliferation and induces apoptosis in vitro[1].
Cell Research Cell lines Solid tumor cells/hematologic cell lines; i.e. Human A549 (lung carcinoma), U2OS (osteosarcoma), HCT116 (colorectal carcinoma), U87MG (glioblastoma), A375 (malignant melanoma), MV-4-11 (biphenotypic B-myelomonocytic leukemia), RPMI 8226 (myeloma), L363 (multiple myeloma) cancer cell lines
Concentrations 0, 0.1, 0.2, 0.4, 0.6, 0.8, 1 μM
Incubation Time 2-72 h
Method Solid tumor cells are plated in poly-d-lysine coated and hematologic cell lines are seeded in noncoated 96-well plates overnight before being treated with compounds. Solid tumor cells are fixed with Prefer for 20 minutes at room temperature and permeated with 0.1% Triton X-100 in PBS for 15 minutes. Caspase-3 expression is measured by immunofluorescence with antiactivated caspase-3. Terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) activity is measured. Hematologic tumor cells are assayed for cell viability.
In Vivo
In vivo LY2857785 inhibits RNAP II CTD Ser2 phosphorylation in vivo. It demonstrates potent antitumor growth efficacy in preclinical tumor models and increases animal survival. No significant weight loss is observed in the nude mouse study while animal mortality is observed in these studies at LY2957785 high-dose groups[1].
Animal Research Animal Models female nude rats or athymic nude female mice
Dosages 4, 8, 12 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 448.60 Formula

C26H36N6O
CAS No. 1619903-54-6 SDF Download LY2857785 SDF
Smiles CC(C)C1=C2C=C(C=CC2=NN1C)C3=NC(=NC=C3)NC4CCC(CC4)NC5CCOCC5
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 42 mg/mL

DMSO : 23 mg/mL ( (51.27 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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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

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