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Cell Cycle/Checkpoint CDK LY2857785

LY2857785

Catalog No. TQ0060   CAS 1619903-54-6
Purity 98.00% Datasheet

LY2857785 is a type I competitive and reversible ATP kinase inhibitor against CDK7/CDK8/CDK9 (IC50s: 246 nM/16 nM/11 nM).

LY2857785, CAS 1619903-54-6
Pack Size Availability Price/USD Quantity
10 mg Inquiry 379.00
25 mg Inquiry 782.00
50 mg Inquiry 1264.00
100 mg Inquiry 2265.00
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description LY2857785 is a type I competitive and reversible ATP kinase inhibitor against CDK7/CDK8/CDK9 (IC50s: 246 nM/16 nM/11 nM).
Targets&IC50
Kinase Assay CDK7 and CDK9 reaction mixtures contain 10 mM Tris-HCl (pH 7.4), 10 mM HEPES, 5 mM DTT, 10 μM ATP, 0.5 μCi 33p-ATP, 10 mM MnCl2, 150 mM NaCl, 0.01% Triton X-100, 2% DMSO, 0.05 mM CDK7/9ptide, and 2 nM CDK7/Mat1/cyclin H, or 2 nM CDK9/cyclin T1, respectively. CDK8/cyclin C reaction is performed in HEPES 30 mM, DTT 2 mM, MgCl2 5 mM, 0.015% Triton X-100, 5 μM ATP, and 400 nM of RBER-CHKStide containing 20 nM of enzyme. LY2857785 in DMSO is diluted serially 1:3 for dose-response. Reactions are carried out in 96-well polystyrene plates. The reactions are incubated at room temperature for 60 minutes and followed by termination with 10% H3PO4 or 10% trichloroacetic acid (TCA). For the filter binding assay, reactions are transferred to 96-well filter plates and measured by Microbeta scintillation counter. For ADP Transcreener Fluorescent Polarization Assays, reactions are quenched with ADP detection mix, incubated 2 hours at room temperature and then FP is measured at λex=610 nm, λem=670 nm on a Tecan Ultra 384 plate reader. The concentration of ADP product is calculated from millipolarization (μP) using a prepared ADP/ATP dilution series as a standard curve. Kinase profiling are carried out in 96-well polystyrene plates. Briefly, in a final volume of 25 μL the enzyme is incubated with the appropriate buffer, peptide substrate, and the diluted LY2857785. Reactions are initiated by the addition of ATP/[33P] and the ATP mix is incubated at room temperature for 40 minutes. Reactions are quenched with the addition of 5 μL of 3% phosphoric acid, 10 μL of the reaction are spotted onto a filter mat, washed 3 times for 5 minutes in 75 mM phosphoric acid and once in methanol. Once the filters are dry, they are submitted to scintillation counting.
Cell Research
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 LY2857785. 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 anti-activated caspase-3. Terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) activity is measured with In Situ Cell Death Detection Kit. Both assays are analyzed on Acumen Explorer laser-scanning fluorescence microplate cytometer. Hematologic tumor cells are assayed for cell viability with CellTiter-Glo Luminescent Cell Viability Assay.
Animal Research
For xenograft models, human cancer cells A375, U87MG, MV-4-11, and HCT116 are implanted into female nude rats or athymic nude female mice. The animals are dosed with saline, Rapamycin, or LY2857785, respectively. MV-4-11 xenografts in nude mice are treated by LY2857785 (4, 8, and 18 mg/kg) i.v. bolus. MV-4-11 xenografts in nude rats are treated with LY2857785 (3, 6, and 9 mg/kg) 4-hour i.v. infusion. An untreated vehicle control group is administered saline i.v. every 3 days. Flow cytometry analysis is conducted using Beckman Coulter's CXP software. Statistical significance of the effect of LY2857785 and/or control compounds is assessed by the Dunnett method, one-way ANOVA.
Synonyms
Purity 98.00%
Appearance solid
Molecular Weight 448.60
Formula C26H36N6O
CAS No. 1619903-54-6

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

:

DMSO: 10mg/mL(22.29 mM; Need ultrasonic)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Yin T, et al. A novel CDK9 inhibitor shows potent antitumor efficacy in preclinical hematologic tumor models. Mol Cancer Ther. 2014 Jun;13(6):1442-56. Mol Cancer Ther. 2014 Jun;13(6):1442-56.

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