TG101348 (SAR302503)JAK-2 inhibitor,potent and selective CAS# 936091-26-8 |
Quality Control & MSDS
3D structure
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| Cas No. | 936091-26-8 | SDF | Download SDF |
| PubChem ID | 16722836 | Appearance | Powder |
| Formula | C27H36N6O3S | M.Wt | 524.68 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Fedratinib; SAR 302503 | ||
| Solubility | DMSO : ≥ 42 mg/mL (80.05 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-tert-butyl-3-[[5-methyl-2-[4-(2-pyrrolidin-1-ylethoxy)anilino]pyrimidin-4-yl]amino]benzenesulfonamide | ||
| SMILES | CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)OCCN4CCCC4 | ||
| Standard InChIKey | JOOXLOJCABQBSG-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C27H36N6O3S/c1-20-19-28-26(30-21-10-12-23(13-11-21)36-17-16-33-14-5-6-15-33)31-25(20)29-22-8-7-9-24(18-22)37(34,35)32-27(2,3)4/h7-13,18-19,32H,5-6,14-17H2,1-4H3,(H2,28,29,30,31) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. | |||||
| Targets | JAK2 | |||||
| IC50 | 3 nM | |||||
| Kinase experiment [1]: | |
| Inhibitory activities | IC50 values for TG101348 were determined commercially using the InVitrogen kinase profiling service for a 223 kinase screen that included JAK2 and JAK2V617F or Carna Biosciences for the screen of all Janus kinase family members including JAK1 and Tyk2. ATP concentration was set to approximately the Km value for each kinase. |
| Cell experiment [1]: | |
| Cell lines | Human erythroleukemic cell line (HEL) with JAK2V617F mutation; Ba/F3 cells |
| Preparation method | Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
| Reacting condition | 0.1, 0.3, 1, 3, and 10 μM; 72 h. |
| Applications | In HEL and Ba/F3 cells with JAK2V617F mutation, TG101348 (SAR302503) inhibits cell proliferation with IC50 values of 300 nM and 420 nM, respectively. TG101348 also reduces STAT5 phosphorylation and induces apoptosis in a dose-dependent way. |
| Animal experiment [1]: | |
| Animal models | C57Bl/6 mice; C57BL/6 mice intravenously injected with whole bone marrow expressing JAK2V617F. |
| Dosage form | 30, 100, and 200 mg/kg; 0.5, 1, 3, 5, 7, and 24 hr postdose; administrated orally.60 mg/kg, 120 mg/kg; oral gavage twice daily; from day 28 on for 42 days. |
| Application | In C57Bl/6 mice, maximum plasma concentrations (Cmax) of TG101348 are 0.68, 3.58, and 4.28 μM at 3 h postdose at doses 30, 100, and 200 mg/kg, respectively. In mice with polycythemia vera induced by JAK2V617F, TG101348 reduces hematocrit by 5.1% and 17.9% at 60 mg/kg and 120 mg/kg, respectively. Also, TG101348 dose-dependently inhibits splenomegaly and polycythemia. |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1]. Wernig G, Kharas MG, Okabe R, et al. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell, 2008, 13(4): 311-320. | |
TG101348 (SAR302503) Dilution Calculator
TG101348 (SAR302503) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.9059 mL | 9.5296 mL | 19.0592 mL | 38.1185 mL | 47.6481 mL |
| 5 mM | 0.3812 mL | 1.9059 mL | 3.8118 mL | 7.6237 mL | 9.5296 mL |
| 10 mM | 0.1906 mL | 0.953 mL | 1.9059 mL | 3.8118 mL | 4.7648 mL |
| 50 mM | 0.0381 mL | 0.1906 mL | 0.3812 mL | 0.7624 mL | 0.953 mL |
| 100 mM | 0.0191 mL | 0.0953 mL | 0.1906 mL | 0.3812 mL | 0.4765 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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TG101348, also known as SAR302503, is a potent and selective inhibitor of janus kinase 2 (JAK2), one member of a family of 4 cytoplasmic tyrosine kinases including janus kinase 1(JAK1), JAK2, janus kinase 3 (JAK3) and tyrosine kinase 2 (Tyk2), with the inhibition constant IC50 of 3 nM. Comparing to other close related kinases, the selectivity of TG101348 for JAK2 is 35- and 334-fold stronger than that for JAK3 and JAK1 respectively. TG10348 is capable of inducing apoptosis in HEL cells as well BaF/3 cells harboring JAK2V617 mutation and inhibiting hematopoietic progenitor colony formation and erythroid engraftment in samples from polycythemia vera (PV) patients.
Reference
Srdan Verstovsek. Therapeutic potential of JAK2 inhibitors. Hematology Am Soc Hematol Educ Program 2009:636-642
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