TG101209 |
| Catalog No.GC10035 |
An inhibitor of JAK2, FLT3, RET, and JAK3
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 936091-14-4
Sample solution is provided at 25 µL, 10mM.
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TG101209, a small-molecule identified by structure based design, is a selective inhibitor of janus kinase 2 (Jak2) that potently inhibits Jak/Stat pathway in multiple myeloma (MM) cell lines, such as cell harboring JAK2V617F or MPLW515L/K mutations which are commonly associated with polycythemia vera (PV) and primary myelofibrosis (PMF) respectively. According to results of multiple studies, it has revealed that TG101209 exhibits a dose and time dependent cyctoxicity, which is associated with inhibited cell cycle progrgression and induced apoptosis, in a wild range of MM cell lines through suppressing the expression of pJak2, pStat3 and Bcl-xl and inducing the overexpression of pErk and pAkt.
Reference
[1].Ramakrishnan V, Kimlinger T, Haug J, Timm M, Wellik L, Halling T, Pardanani A, Tefferi A, Rajkumar SV, Kumar S. TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells. Am J Hematol. 2010;85(9):675-686.
Cell experiment: | 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. |
Animal experiment: | 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). |
References: [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. | |
| Cas No. | 936091-14-4 | SDF | |
| Chemical Name | N-tert-butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide | ||
| Canonical SMILES | CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)N4CCN(CC4)C | ||
| Formula | C26H35N7O2S | M.Wt | 509.67 |
| Solubility | ≥ 25.5 mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9621 mL | 9.8103 mL | 19.6205 mL |
| 5 mM | 0.3924 mL | 1.9621 mL | 3.9241 mL |
| 10 mM | 0.1962 mL | 0.981 mL | 1.9621 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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