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LY2857785 CDK inhibitor

Name: LY2857785
Brand: Selleck Chemicals
SKU: S7511
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S7511

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

Chemical Structure

Molecular Weight: 448.60

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

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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Chemical Information, Storage & Stability

Molecular Weight	448.60	Formula	C₂₆H₃₆N₆O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1619903-54-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)C1=C2C=C(C=CC2=NN1C)C3=NC(=NC=C3)NC4CCC(CC4)NC5CCOCC5

Solubility

In vitro
Batch:

Ethanol : 42 mg/mL

DMSO : 23 mg/mL (51.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.4mg/ml (0.89mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.4mg/ml (0.89mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	CDK9 ^[1] (Cell-free assay) 0.011 μM CDK8 ^[1] (Cell-free assay) 0.016 μM CDK7 ^[1] (Cell-free assay) 0.246 μM
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, this compound inhibits CTD P-Ser2 and CTD P-Ser5 in U2OS cells at IC50s 0.089 and 0.042 μM. Although it 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 this chemical only induces a moderate G2–M DNA content increase, from 35% to 55%, with EC50 0.135 μmol/L. It inhibits hematologic and solid tumor cell proliferation and induces apoptosis in vitro^[1].
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 this compound high-dose groups^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/24688048/

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