TG101209
Based on 5 publication(s) in Google Scholar
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
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- Pureza: 98.13%
- No. CAS: 936091-14-4
- Fòrmula: C26H35N7O2S
- Peso molecular:509.67
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TG101209
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Actividad biológica
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JAK2 6 nM (IC50) |
JAK3 169 nM (IC50) |
RET 17 nM (IC50) |
FLT3 25 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
170 nM
Compound: TG101209
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Cytotoxicity against mouse BaF3 cells harboring EPOR JAK2 V617F mutant measured after 24 hrs by XTT assay
Cytotoxicity against mouse BaF3 cells harboring EPOR JAK2 V617F mutant measured after 24 hrs by XTT assay
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[PMID: 36805946] |
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 200 nM. In a human JAK2V617F-expressing acute myeloid leukemia cell line, TG101209 induces 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 triggers apoptosis of transformed Ba/F3 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 936091-14-4
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Appearance Solid
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Peso molecular 509.67
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Fòrmula C26H35N7O2S
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Color White to gray
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SMILES
O=S(C1=CC=CC(NC2=NC(NC3=CC=C(C=C3)N4CCN(CC4)C)=NC=C2C)=C1)(NC(C)(C)C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Biomed Pharmacother
C-CBL is required for inhibition of angiogenesis through modulating JAK2/STAT3 activity in ROP development. [Abstract]2020 Dec;132:110856. PMID: 33125970 -
Elife
Metal environmental contamination within different human exposure context- specific and non-specific biomarkers. [Abstract]2020 May 15;324:46-53. PMID: 31935480 -
Eur J Pharmacol
Autocrine secretion of insulin-like growth factor-I mediates growth hormone-stimulated DNA synthesis and proliferation in primary cultures of adult rat hepatocytes. [Abstract]2021 Jan 15;891:173753. PMID: 33245901 -
J Pharm Pharm Sci
Growth Hormone Signaling Pathway Leading to the Induction of DNA Synthesis and Proliferation in Primary Cultured Hepatocytes of Adult Rats. [Abstract]2021:24:1-15. PMID: 33434118 -
J Dermatol Sci
The role and mechanism of JAK2 inhibitor in endothelial mesenchymal transition in systemic sclerosis. [Abstract]2025 Mar;117(3):71-80. PMID: 40023747
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (98.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (5.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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 inhibits proliferation by 50%. All experiments are done in triplicate and the results normalized to growth of untreated cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Severe combined immunodeficiency (SCID) mice are intravenously injected with 10 times 106 sorted GFP-positive BaF/3 cells expressing JAK2V617F (Ba/F3-V617F-GFP). TG101209 is administered by oral gavage at the indicated doses beginning day +3 after tumor cell infusion and ending on day +20. On day +11 following tumor cell injection, 1 mL blood is collected by terminal cardiac bleeding from the mouse that receives vehicle, and 0.1 mL of blood is collected by non-lethal retro-orbital collection from each of the three six-mouse groups dosed with 10, 30 or 100 mg/kg b.i.d. (twice daily) of TG101209, and samples pooled within the dose groups. Blood mononuclear cells are isolated by a Ficoll cushion centrifugation method (600 RCF and 30 min). The isolated cells are subjected to FACS analysis to determine the percentage of GFP-positive tumor cells (that is, Ba/F3-V617F-GFP cells).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Pardanani A, et al. TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia. 2007 Aug;21(8):1658-68. [Content Brief]
[2]. Ma AC, et al. A novel zebrafish jak2a(V581F) model shared features of human JAK2(V617F) polycythemia vera. Exp Hematol. 2009 Dec;37(12):1379-1386.e4. [Content Brief]
[3]. Sun Y, et al. Inhibition of JAK2 signaling by TG101209 enhances radiotherapy in lung cancer models. J Thorac Oncol. 2011 Apr;6(4):699-706 [Content Brief]
[4]. Cuesta-Dominguez A, et al. Transforming and tumorigenic activity of JAK2 by fusion to BCR: molecular mechanisms of action of a novel BCR-JAK2 tyrosine-kinase. PLoS One. 2012;7(2):e3245 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9621 mL | 9.8103 mL | 19.6205 mL | 49.0513 mL |
| 5 mM | 0.3924 mL | 1.9621 mL | 3.9241 mL | 9.8103 mL | |
| 10 mM | 0.1962 mL | 0.9810 mL | 1.9621 mL | 4.9051 mL | |
| 15 mM | 0.1308 mL | 0.6540 mL | 1.3080 mL | 3.2701 mL | |
| 20 mM | 0.0981 mL | 0.4905 mL | 0.9810 mL | 2.4526 mL | |
| 25 mM | 0.0785 mL | 0.3924 mL | 0.7848 mL | 1.9621 mL | |
| 30 mM | 0.0654 mL | 0.3270 mL | 0.6540 mL | 1.6350 mL | |
| 40 mM | 0.0491 mL | 0.2453 mL | 0.4905 mL | 1.2263 mL | |
| 50 mM | 0.0392 mL | 0.1962 mL | 0.3924 mL | 0.9810 mL | |
| 60 mM | 0.0327 mL | 0.1635 mL | 0.3270 mL | 0.8175 mL | |
| 80 mM | 0.0245 mL | 0.1226 mL | 0.2453 mL | 0.6131 mL |
TG101209 Related Classifications
HY-10410 Related Classifications
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