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Catalog No. T3065   CAS 936091-14-4

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

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TG101209, CAS 936091-14-4
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Purity: 98%
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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


Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 94 mg/mL (184.4 mM)

Ethanol: <1 mg/mL

H2O: <1 mg/mL

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

References 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:
Anti-Cancer Compound Library Preclinical Compound Library Autophagy Compound Library Anti-Obesity Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Histone Modification Compound Library Immunology/Inflammation Compound Library Anti-Metabolism Disease Compound Library Kinase Inhibitor Library

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TG101209 936091-14-4 JAK/STAT信号通路 表观遗传 蛋白酪氨酸激酶 凋亡 干细胞 血管生成 自噬 Apoptosis Autophagy c-RET FLT JAK Cluster of differentiation antigen 135 RET Inhibitor Janus kinase CD135 Fms like tyrosine kinase 3 TG 101209 FLT3 TG-101209 inhibit inhibitor