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TG101209

Catalog No. T3065   CAS 936091-14-4

TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.

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TG101209 Chemical Structure
TG101209, CAS 936091-14-4
Pack Size Availability Price/USD Quantity
2 mg In stock $ 40.00
5 mg In stock $ 61.00
10 mg In stock $ 85.00
25 mg In stock $ 108.00
50 mg In stock $ 126.00
100 mg In stock $ 207.00
1 mL * 10 mM (in DMSO) In stock $ 67.00
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Purity: 100%
Purity: 99%
Purity: 98.81%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
Targets&IC50 JAK2:6 nM
Kinase Assay Cell-free Kinase Activity Assays: IC50 values for TG101209 are determined using a luminescence-based kinase assay with recombinant JAK2, VEGFR2/KDR, and JAK3 obtained from Upstate Cell Signaling Solutions. Kinase reactions are carried out in a buffer consisting of 40 mM Tris buffer (pH 7.4), 50 mM MgCl2, 800?M EGTA, 350?M Triton X-100, 2?M ?-mercaptoethanol, 100?M peptide substrate, and an appropriate amount of JAK2, VEGFR2/KDR or JAK3 such that the assay is linear over 60 minutes. The reaction is initiated by the addition of 10?L of ATP to a final concentration of 3 mM and terminated by the addition of Kinase-Glo reagent after 60 minutes. Luciferase activity is quantified using an Ultra 384 instrument set for luminosity measurements. IC50 values are derived from experimental data using the non-linear curve fitting capabilities of the GraphPad Prism 4.0 software. The single concentration inhibition data for a panel of 63 kinases is determined using the SelectScreen TM service.
Cell Research In brief, approximately 2 × 103 cells are plated into microtiterplate wells in 100 ml RPMI-1640 growth media with indicated concentrations of TG101209. The relative growth of cells is quantified at 24-hour intervals using Cell Proliferation Kit II (XTT) as per manufacturer's guidelines. After incubation, 20 mL of XTT is added to the wells and allowed to incubate for 4-6 hours. The colored formazan product is measured spectrophotometrically at 450 nm with correction at 650 nm, and IC50 values are determined using the GraphPad Prism 4.0 software. Data are subjected to a non-linear regression-fit analysis and IC50 values are determined as the concentration that inhibited proliferation by 50%. All experiments are done in triplicate and the results normalized to growth of untreated cells.(Only for Reference)
Molecular Weight 509.67
Formula C26H35N7O2S
CAS No. 936091-14-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 94 mg/mL (184.4 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Pardanani A, et al, Leukemia, 2007, 21(8), 1658-1668. 2. Ma AC, et al, Exp Hematol, 2009, 37(12), 1379-1386. 3. Sun Y, et al, J Thorac Oncol, 2011, 6(4), 699-706. 4. Cuesta-Dominquez A, et al, PLoS One, 2012, 7(2), e32451. 5. Wang Y, et al, Blood, 2009, 114(24), 5024-5033.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Hematonosis Compound Library Bioactive Compounds Library Max Reprogramming Compound Library JAK-STAT Compound Library Anti-Diabetic Compound Library Anti-Aging Compound Library Kinase Inhibitor Library Inhibitor Library Apoptosis Compound Library

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Keywords

TG101209 936091-14-4 Angiogenesis Apoptosis Autophagy Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors JAK c-RET FLT Cluster of differentiation antigen 135 RET Inhibitor Janus kinase TG-101209 CD135 Fms like tyrosine kinase 3 FLT3 TG 101209 inhibit inhibitor

 

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