TG101209

For research use only.

Catalog No.S2692

13 publications

TG101209 Chemical Structure

CAS No. 936091-14-4

TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET (c-RET) with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.

Selleck's TG101209 has been cited by 13 publications

3 Customer Reviews

  • EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (*,P < 0.05; **, P < 0.01; ***, P < 0.001; NS, nonsignificant).

    Clin Cancer Res 2014 20(13), 3496-506. TG101209 purchased from Selleck.

  • Primary plasma cells from MM patient 5 used were incubated with indicated concentrations of LCL161, TG101209 or the combination for 24 h. Western blot analysis were performed to examine expression levels of pStat3 and IAPs.

    Leukemia 2014 28(7), 1519-28. TG101209 purchased from Selleck.

  • Claude HAAN Université du Luxembour. TG101209 purchased from Selleck.

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Biological Activity

Description TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET (c-RET) with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.
Targets
JAK2 [1]
(Cell-free assay)		 RET [1]
(Cell-free assay)		 FLT3 [1]
(Cell-free assay)		 JAK3 [1]
(Cell-free assay)
6 nM 17 nM 25 nM 169 nM
In vitro

TG101209 is an orally bioavailable, small molecule, ATP-competitive inhibitor towards several tyrosine kinases. TG101209 inhibits growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 of B200 nM. In a human JAK2V617F-expressing acute myeloid leukemia cell line, TG101209 inducs cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3. TG101209 suppresses growth of hematopoietic colonies from primary progenitor cells harboring JAK2V617F or MPL515 mutations. [1] TG101209 significantly reduces STAT5 phosphorylation without affecting the total amount of STAT5 protein. [2] TG101209 inhibits survivin and reduces phosphorylation of STAT3 in HCC2429 and H460 lung cancer cells. TG101209 results in radio sensitization of HCC2429 and H460 lung cancer cells in vitro. [3] A recent study indicates TG101209 abrogates BCR-JAK2 and STAT5 phosphorylation, decreases Bcl-xL expression and triggered apoptosis of transformed Ba/F3 cells. [4]

In vivo 100 mg/kg of TG101209 effectively prolongs the survival in JAK2V617F-induced disease (10 days). Compared with placebo-treated animals, TG101209-treated animals exhibit statistically significant, dose-dependent reduction in the circulating tumor cell burden at day +11 to 20%. [1]

Protocol

Kinase Assay:[1]
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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 40mM Tris buffer (pH 7.4), 50mM 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 3mM 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:[1]
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  • Cell lines: Ba/F3 cells expressing JAK2V617F (Ba/F3-EpoR-V617F) and MPLW515L (Ba/F3-W515L) mutants.
  • Concentrations: 4.6-38 400 nM
  • Incubation Time: 28-30 hours
  • Method: 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)
Animal Research:[1]
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  • Animal Models: Ba/F3-V617F-GFP cells are injected into immunodeficient SCID mice to induce a rapidly fatal, fully penetrant hematopoietic disease.
  • Dosages: 100 mg/kg
  • Administration: TG101209 is administered via oral gavage at the indicated doses beginning day +3 after tumor cell infusion and ending on day +20.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 102 mg/mL (200.12 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing. 		12 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 509.67
Formula

C26H35N7O2S
CAS No. 936091-14-4
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)N4CCN(CC4)C

In vivo Formulation Calculator (Clear solution)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID