Fedratinib hydrochloride hydrate (Synonyms: TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate) |
| Catalog No.GC60161 |
페드라티닙 염산염 수화물(TG-101348 염산염 수화물)은 JAK2 및 JAK2V617F 키나제 모두에 대해 IC50이 3nM인 강력하고 선택적인 ATP 경쟁적 경구 활성 JAK2 억제제입니다. 페드라티닙 염산염 수화물은 JAK1 및 JAK3에 비해 각각 35배 및 334배 선택성을 나타냅니다. 페드라티닙 염산염 수화물은 암세포의 세포자살을 유도하고 골수증식성 장애 연구에 대한 잠재력을 가지고 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1374744-69-0
Sample solution is provided at 25 µL, 10mM.
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Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research[1][2].
Fedratinib (TG101348) inhibits proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with an IC50 value of approximately 300 nM for either line. Proliferation of parental Ba/F3 cells was inhibited to a comparable level, with an IC50 value of ∼420 nM[1]. Exposure of these cells to Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation[1]. Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner[1].
Fedratinib (TG101348; 60-120 mg/kg; oral gavage; twice daily; for 42 days; C57Bl/6 mice) trewatment shows a dose-dependent reduction in polycythemia and a marked dose-dependent reduction in splenomegaly of treated animals[1]. Animal Model: C57Bl/6 mice induced by the JAK2V617F mutation[1]
[1]. Wernig G, et al. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell. 2008 Apr;13(4):311-20. [2]. Geron I, et al. Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitors. Cancer Cell. 2008 Apr;13(4):321-30.
| Cas No. | 1374744-69-0 | SDF | |
| Synonyms | TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate | ||
| Canonical SMILES | [H]Cl.[H]O[H].[H]Cl.O=S(C1=CC=CC(NC2=NC(NC3=CC=C(C=C3)OCCN4CCCC4)=NC=C2C)=C1)(NC(C)(C)C)=O | ||
| Formula | C27H40Cl2N6O4S | M.Wt | 615.62 |
| Solubility | DMSO: 250 mg/mL (406.09 mM) | 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 | 1.6244 mL | 8.1219 mL | 16.2438 mL |
| 5 mM | 0.3249 mL | 1.6244 mL | 3.2488 mL |
| 10 mM | 0.1624 mL | 0.8122 mL | 1.6244 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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