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TG101209

Cat. No. M1887
TG101209 Structure
Size Price Availability Quantity
10mg USD 130 In stock
50mg USD 400 In stock
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Quality Control
Biological Activity

TG101209, an orally bioavailable JAK2 inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. TG101209 potently inhibits JAK2 (IC(50)=6 nM), FLT3 (IC(50)=25 nM) and RET (IC(50)=17 nM) kinases, with significantly less activity against other tyrosine kinases including JAK3 (IC(50)=169 nM). TG101209 also inhibited STAT3 activation and survivin expression, and sensitized HCC2429 (DER=1.34, p=0.002) and H460 (DER=1.09, p=0.006) cells to radiation in clonogenic assays. In vivo, addition of TG101209 to radiation in lung xenografts produced a significant tumor growth delay (>10 days). TG101209 has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells.

Protocol
Cell Experiment
Cell lines Ba/F3 cells, MPLW515L, CTLL-2 cells and HEL and K562 cells
Preparation method XTT assay for cell proliferation.
In brief, approximately 2*103 cells were plated into microtiterplate wells in 100 ml RPMI-1640 growth media with indicated concentrations of inhibitor. The relative growth of cells was quantified at 24-h intervals using Cell Proliferation Kit II (XTT) as per manufacturer’s guidelines (Roche, Indianapolis, IN, USA). After incubation, 20 ml of XTT was added to the wells and allowed to incubate for 4–6 h. The colored formazan product was measured spectrophotometrically at 450 nm with correction at 650 nm, and IC50 values were determined using the GraphPad Prism 4.0 software. Data were subjected to a non-linear regression-fit analysis and IC50 values were determined as the concentration, that inhibited proliferation by 50%. All experiments were done in triplicate and the results normalized to growth of untreated cells.
Concentrations 0~100 μ M
Incubation time 24 h
Animal Experiment
Animal models JAK2V617F-induced hematopoietic disease in a nude mouse model
Formulation DMSO
Dosages 10, 30 and 100mg/kg bid
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 509.67
Formula C26H35N7O2S
CAS Number 936091-14-4
Purity 99.01%
Solubility DMSO 100 mg/mL
Storage at -20°C
References

TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells.
Ramakrishnan V, et al. Am J Hematol. 2010 Sep;85(9):675-86. PMID: 20652971.

TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations.
Pardanani A, et al. Leukemia. 2007 Aug;21(8):1658-68. PMID: 17541402.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TG101209 supplier, JAK, inhibitors

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