Fedratinib
Based on 54 publication(s) in Google Scholar
Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 936091-26-8
- Formula: C27H36N6O3S
- Molecular Weight:524.68
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Fedratinib
More- Signal Transduct Target Ther. 2022 Feb 23;7(1):52. [Abstract]
- Signal Transduct Target Ther. 2020 Dec 26;5(1):295. [Abstract]
- Nature. 2023 Jun;618(7963):151-158. [Abstract]
- Science. 2026 Feb 5;391(6785):eadz4075. [Abstract]
- Cell. 2024 Apr 25;187(9):2288-2304.e27. [Abstract]
- Mol Cancer. 2023 May 20;22(1):86. [Abstract]
- Mol Cancer. 2021 May 29;20(1):80. [Abstract]
- Nat Cell Biol. 2026 Mar 13. [Abstract]
- Nat Commun. 2025 Sep 29;16(1):8560. [Abstract]
- J Adv Res. 2026 Apr 24:S2090-1232(26)00358-9. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Nanobiotechnology. 2025 Oct 10;23(1):649. [Abstract]
- J Exp Clin Cancer Res. 2025 Jan 2;44(1):2. [Abstract]
- J Neuroinflammation. 2022 Oct 10;19(1):253. [Abstract]
- Mol Ther Oncol. 2024 Jun 07.
- NPJ Breast Cancer. 2026 Feb 12. [Abstract]
- Free Radic Biol Med. 2026 Apr:247:486-501. [Abstract]
- Cell Prolif. 2020 Feb;53(2):e12742. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- J Med Chem. 2021 Feb 25;64(4):2228-2241. [Abstract]
- Am J Clin Nutr. 2020 Jan 1;111(1):110-121. [Abstract]
- Cancer Cell Int. 2021 Jun 5;21(1):291. [Abstract]
- Mol Ther Nucleic Acids. 2020 Sep 4;21:900-915. [Abstract]
- Life Sci. 2023 May 15:321:121608. [Abstract]
- EMBO Rep. 2019 Jun;20(6):e47202. [Abstract]
- Cancer Biol Ther. 2024 Dec 31;25(1):2432117. [Abstract]
- Int Immunopharmacol. 2023 Oct 19;125(Pt A):111087. [Abstract]
- Int J Mol Sci. 2023 May 25;24(11):9243. [Abstract]
- Invest Ophthalmol Vis Sci. 2024 Sep 3;65(11):21. [Abstract]
- Molecules. 2018 Aug 18;23(8). pii: E2071. [Abstract]
- Sci Rep. 2025 Jan 24;15(1):3124. [Abstract]
- Mol Pharm. 2017 Jan 3;14(1):274-283. [Abstract]
- Mol Cell Biochem. 2025 Apr;480(4):2645-2660. [Abstract]
- FASEB J. 2026 Apr 30;40(8):e71804. [Abstract]
- BMC Cancer. 2022 Aug 13;22(1):885. [Abstract]
- J Pharm Sci. 2025 Feb;114(2):1444-1454. [Abstract]
- Toxicol Appl Pharmacol. 2024 Dec 24:495:117216. [Abstract]
- Neuropsychiatr Dis Treat. 2020 Apr 1;16:891-900. [Abstract]
- IUBMB Life. 2018 Jan;70(1):81-91. [Abstract]
- Mol Pharmacol. 2022 Jun;101(6):381-389. [Abstract]
- bioRxiv. 2026 Feb 18:2026.02.16.706212. [Abstract]
- bioRxiv. 2025 Nov 26.
- University of Pennsylvania. 2025.
- SSRN. 2025 Jul 4.
- bioRxiv. 2025 February 21.
- bioRxiv. 2024 September 24.
- University of Michigan. 2024.
- Biomed Pharmacother. 2024 May:174:116447. [Abstract]
- bioRxiv. 2024 Nov 5:2024.02.02.578646. [Abstract]
- University of Michigan. 2023 Sep.
- bioRxiv. 2024 May 6:2023.06.07.544058. [Abstract]
- Patent. US20210128545A1.
- University of California. 2021 Apr.
- Research Square Preprint. 2020 Jun.
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WB
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IF
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Cell Proliferation/Viability Assay
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WB
Biological Activity
|
JAK2 3 nM (IC50) |
JAK2(V617F) 3 nM (IC50) |
Flt3 15 nM (IC50) |
Ret 48 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.56 μM
Compound: Fedratinib
|
Antiproliferative activity against human A549 cells
Antiproliferative activity against human A549 cells
|
[PMID: 37875056] |
| A549 | IC50 |
1.73 μM
Compound: Fedratinib
|
Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 37057760] |
| A549 | IC50 |
1.73 μM
Compound: Fedratinib
|
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
|
[PMID: 38964169] |
| BaF3 | IC50 |
270 nM
Compound: 32
|
Antiproliferative activity against mouse BaF3 cells harboring JAK2 V617F mutant assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
Antiproliferative activity against mouse BaF3 cells harboring JAK2 V617F mutant assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
|
[PMID: 32120325] |
| BaF3 | IC50 |
300 nM
Compound: 25
|
Antiproliferative activity against mouse BaF3 cells harboring JAK2 V617F mutant assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
Antiproliferative activity against mouse BaF3 cells harboring JAK2 V617F mutant assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
|
[PMID: 35749986] |
| BaF3 | IC50 |
420 nM
Compound: 32
|
Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
|
[PMID: 32120325] |
| GES1 | IC50 |
0.61 μM
Compound: TG101348
|
Cytotoxicity against human GES1 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of SAHA by MTT assay
Cytotoxicity against human GES1 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of SAHA by MTT assay
|
[PMID: 37796543] |
| GES1 | IC50 |
0.89 μM
Compound: TG101348
|
Cytotoxicity against human GES1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human GES1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 37796543] |
| HEL | IC50 |
2.01 μM
Compound: Fedratinib
|
Antiproliferative activity against HEL cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against HEL cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 37057760] |
| HEL | IC50 |
300 nM
Compound: 25
|
Antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
Antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
|
[PMID: 35749986] |
| HEL | IC50 |
305 nM
Compound: 32
|
Antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
Antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
|
[PMID: 32120325] |
| HeLa | IC50 |
2.69 μM
Compound: Fedratinib
|
Antiproliferative activity against human HeLa cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 37057760] |
| HepG2 | IC50 |
0.56 μM
Compound: Fedratinib
|
Antiproliferative activity against human HepG2 cells
Antiproliferative activity against human HepG2 cells
|
[PMID: 37875056] |
| HL-60 | IC50 |
4.66 μM
Compound: Fedratinib
|
Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 37057760] |
| Jurkat | IC50 |
0.56 μM
Compound: Fedratinib
|
Antiproliferative activity against human Jurkat cells
Antiproliferative activity against human Jurkat cells
|
[PMID: 37875056] |
| K562 | IC50 |
1.47 μM
Compound: Fedratinib
|
Antiproliferative activity against human K562 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human K562 cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 37057760] |
| MCF7 | IC50 |
4.16 μM
Compound: Fedratinib
|
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 37057760] |
| MDA-MB-231 | IC50 |
0.46 μM
Compound: TG101348
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of SAHA by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of SAHA by MTT assay
|
[PMID: 37796543] |
| MDA-MB-231 | IC50 |
0.56 μM
Compound: Fedratinib
|
Antiproliferative activity against human MDA-MB-231 cells
Antiproliferative activity against human MDA-MB-231 cells
|
[PMID: 37875056] |
| MDA-MB-231 | IC50 |
1.4 μM
Compound: TG101348
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 37796543] |
| MM1.S | IC50 |
1 μM
Compound: TG101348
|
Antiproliferative activity against human MM1S cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human MM1S cells after 72 hrs by trypan blue exclusion assay
|
[PMID: 28280261] |
| MOLM-13 | IC50 |
69 nM
Compound: 25
|
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as inhibition of cell growth
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as inhibition of cell growth
|
[PMID: 35749986] |
| MV4-11 | EC50 |
79 nM
Compound: TG101348
|
Antiproliferative activity against human MV4-11 cells after 72 hrs by celltiter-blue assay
Antiproliferative activity against human MV4-11 cells after 72 hrs by celltiter-blue assay
|
[PMID: 28280261] |
| MV4-11 | IC50 |
57 nM
Compound: 25
|
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as inhibition of cell growth
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as inhibition of cell growth
|
[PMID: 35749986] |
| PC-3 | IC50 |
1.72 μM
Compound: Fedratinib
|
Antiproliferative activity against human PC-3 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human PC-3 cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 37057760] |
| Vero C1008 | CC50 |
>900 nM
Compound: 18; TG101348, SAR302503
|
Cytotoxicity against African green monkey Vero E6 cells
Cytotoxicity against African green monkey Vero E6 cells
|
[PMID: 33539089] |
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].
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.
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Animal Model:C57Bl/6 mice induced by the JAK2V617F mutation[1]
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Dosage:60 mg/kg, 120 mg/kg
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Administration:Oral gavage; twice daily; for 42 days
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Result:Showed a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 936091-26-8
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Appearance Solid
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Molecular Weight 524.68
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Formula C27H36N6O3S
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Color White to light yellow
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SMILES
O=S(C1=CC=CC(NC2=NC(NC3=CC=C(C=C3)OCCN4CCCC4)=NC=C2C)=C1)(NC(C)(C)C)=O
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Synonyms
TG-101348; SAR 302503
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (54)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Targeting polarized phenotype of microglia via IL6/JAK2/STAT3 signaling to reduce NSCLC brain metastasis. [Abstract]2022 Feb 23;7(1):52. PMID: 35194016 -
Signal Transduct Target Ther
STAT3 ameliorates cognitive deficits by positively regulating the expression of NMDARs in a mouse model of FTDP-17. [Abstract]2020 Dec 26;5(1):295. PMID: 33361763 -
Nature
2023 Jun;618(7963):151-158. PMID: 37198494 -
Science
2026 Feb 5;391(6785):eadz4075. PMID: 41643022 -
Cell
Cancer SLC6A6-mediated taurine uptake transactivates immune checkpoint genes and induces exhaustion in CD8+ T cells. [Abstract]2024 Apr 25;187(9):2288-2304.e27. PMID: 38565142 -
Mol Cancer
The phospholipid transporter PITPNC1 links KRAS to MYC to prevent autophagy in lung and pancreatic cancer. [Abstract]2023 May 20;22(1):86. PMID: 37210549 -
Mol Cancer
GM-CSF mediates immune evasion via upregulation of PD-L1 expression in extranodal natural killer/T cell lymphoma. [Abstract]2021 May 29;20(1):80. PMID: 34051805 -
Nat Cell Biol
2026 Mar 13. PMID: 41826695 -
Nat Commun
A loss-of-function human ADAR variant activates innate immune response and promotes bowel inflammation. [Abstract]2025 Sep 29;16(1):8560. PMID: 41022715 -
J Adv Res
Long noncoding RNA AFAP1-AS1 aggravates immunotherapy resistance in NSCLC by enhancing JAK2 and TYK2 translation. [Abstract]2026 Apr 24:S2090-1232(26)00358-9. PMID: 42035912 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Nanobiotechnology
Targeting JAK2 with a multifunctional nanoinhibitor for long-lasting anti-inflammatory effects and bone repair. [Abstract]2025 Oct 10;23(1):649. PMID: 41074120 -
J Exp Clin Cancer Res
Gastric cancer-derived exosomal let-7 g-5p mediated by SERPINE1 promotes macrophage M2 polarization and gastric cancer progression. [Abstract]2025 Jan 2;44(1):2. PMID: 39748408 -
J Neuroinflammation
Promoted CD4+ T cell-derived IFN-γ/IL-10 by photobiomodulation therapy modulates neurogenesis to ameliorate cognitive deficits in APP/PS1 and 3xTg-AD mice. [Abstract]2022 Oct 10;19(1):253. PMID: 36217178 -
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NPJ Breast Cancer
JAK/STAT1-interferon-ISGylation networks in breast cancer resistance to inhibitors of FOXM1 and CDK4/6. [Abstract]2026 Feb 12. PMID: 41680190 -
Free Radic Biol Med
Tartrate-Resistant Acid Phosphatase 5 (TRAP/ACP5) aggravates atherosclerosis by regulating macrophage polarization and promoting ferroptosis. [Abstract]2026 Apr:247:486-501. PMID: 41692316 -
Cell Prolif
Blockade of JAK2 protects mice against hypoxia-induced pulmonary arterial hypertension by repressing pulmonary arterial smooth muscle cell proliferation. [Abstract]2020 Feb;53(2):e12742. PMID: 31943454
Fedratinib purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2020 Feb;53(2):e12742. [Abstract]
Hypoxia-induced HPASMC proliferation is suppressed by a JAK2 inhibitor. Western blot analysis of p-JAK2, JAK2, p-STAT3 and STAT3 in HPASMCs.
Fedratinib purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2020 Feb;53(2):e12742. [Abstract]
EdU staining of HPASMCs pre-treated with DMSO or TG for 1 h following 24 h hypoxic exposure. All images were taken at an original magnification of ×400.
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Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
J Med Chem
Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof. [Abstract]2021 Feb 25;64(4):2228-2241. PMID: 33570945 -
Am J Clin Nutr
Drug-nutrient interactions: discovering prescription drug inhibitors of the thiamine transporter ThTR-2 (SLC19A3). [Abstract]2020 Jan 1;111(1):110-121. PMID: 31764942 -
Cancer Cell Int
Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]2021 Jun 5;21(1):291. PMID: 34090418 -
Mol Ther Nucleic Acids
Exosomal Transfer of LCP1 Promotes Osteosarcoma Cell Tumorigenesis and Metastasis by Activating the JAK2/STAT3 Signaling Pathway. [Abstract]2020 Sep 4;21:900-915. PMID: 32810692 -
Life Sci
TRIM21 ubiquitylates GPX4 and promotes ferroptosis to aggravate ischemia/reperfusion-induced acute kidney injury. [Abstract]2023 May 15:321:121608. PMID: 36958437 -
EMBO Rep
Tau accumulation triggers STAT1-dependent memory deficits by suppressing NMDA receptor expression. [Abstract]2019 Jun;20(6):e47202. PMID: 31085626 -
Cancer Biol Ther
LCP1 promotes ovarian cancer cell resistance to olaparib by activating the JAK2/STAT3 signalling pathway. [Abstract]2024 Dec 31;25(1):2432117. PMID: 39588922 -
Int Immunopharmacol
2023 Oct 19;125(Pt A):111087. PMID: 37864908 -
Int J Mol Sci
JAK Signaling Is Critically Important in Cytokine-Induced Viral Susceptibility of Keratinocytes. [Abstract]2023 May 25;24(11):9243. PMID: 37298195 -
Invest Ophthalmol Vis Sci
2024 Sep 3;65(11):21. PMID: 39269368 -
Molecules
Green Tea Catechin Is an Alternative Immune Checkpoint Inhibitor that Inhibits PD-L1 Expression and Lung Tumor Growth. [Abstract]2018 Aug 18;23(8). pii: E2071. PMID: 30126206 -
Sci Rep
Decreased PD-L1 contributes to preeclampsia by suppressing GM-CSF via the JAK2/STAT5 signal pathway. [Abstract]2025 Jan 24;15(1):3124. PMID: 39856320 -
Mol Pharm
Codelivery of Ponatinib and SAR302503 by Active Bone-Targeted Polymeric Micelles for the Treatment of Therapy-Resistant Chronic Myeloid Leukemia. [Abstract]2017 Jan 3;14(1):274-283. PMID: 27957861
Fedratinib purchased from MedChemExpress. Usage Cited in: Mol Pharm. 2017 Jan 3;14(1):274-283. [Abstract]
Effects of AP24534 and SAR302503 combination on BCR-ABL1 kinase and related proteins activity in the existence of IL-3.
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Mol Cell Biochem
Amyloid beta-induced signalling in leptomeningeal cells and its impact on astrocyte response. [Abstract]2025 Apr;480(4):2645-2660. PMID: 39499391 -
FASEB J
Targeting JAK2: Genetic and Pharmacological Inhibition Attenuates Immune-Mediated Liver Injury by Suppressing Proinflammatory Macrophage. [Abstract]2026 Apr 30;40(8):e71804. PMID: 41984049 -
BMC Cancer
Systematic transcriptome profiling of pyroptosis related signature for predicting prognosis and immune landscape in lower grade glioma. [Abstract]2022 Aug 13;22(1):885. PMID: 35964070 -
J Pharm Sci
Advantages of the refined Developability Classification System (rDCS) in early discovery. [Abstract]2025 Feb;114(2):1444-1454. PMID: 39725230 -
Toxicol Appl Pharmacol
Cadmium biphasically impacts the adaptive immune system via regulating mitochondrial activation of hematopoietic stem cells in mice. [Abstract]2024 Dec 24:495:117216. PMID: 39725238 -
Neuropsychiatr Dis Treat
Intracerebral Hemorrhage Induced Brain Injury Is Mediated by the Interleukin-12 Receptor in Rats. [Abstract]2020 Apr 1;16:891-900. PMID: 32308392 -
IUBMB Life
MicroRNA-204 deregulation in lung adenocarcinoma controls the biological behaviors of endothelial cells potentially by modulating Janus kinase 2-signal transducer and activator of transcription 3 pathway. [Abstract]2018 Jan;70(1):81-91. PMID: 29281186
Fedratinib purchased from MedChemExpress. Usage Cited in: IUBMB Life. 2018 Jan;70(1):81-91. [Abstract]
A549 cells are treated with TG101348 (3 nM), BMS-911543 (1.5 nM), and Stattic (2.5 lM) for 24 h, and the conditioned media are collected and applied for tube formation assay in HUVECs.
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Mol Pharmacol
Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]2022 Jun;101(6):381-389. PMID: 35383108 -
bioRxiv
Radiation synergizes with BET inhibition to stimulate durable, systemic anti-tumor immunity in murine cancer models. [Abstract]2026 Feb 18:2026.02.16.706212. PMID: 41757027 -
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Biomed Pharmacother
Inhibition the ubiquitination of ENaC and Na,K-ATPase with erythropoietin promotes alveolar fluid clearance in sepsis-induced acute respiratory distress syndrome. [Abstract]2024 May:174:116447. PMID: 38518606 -
bioRxiv
BRD4-mediated epigenetic regulation of endoplasmic reticulum-mitochondria contact sites is governed by the mitochondrial complex III. [Abstract]2024 Nov 5:2024.02.02.578646. PMID: 38352460 -
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bioRxiv
Combination fedratinib and venetoclax has activity against human B-ALL with high FLT3 expression. [Abstract]2024 May 6:2023.06.07.544058. PMID: 37333339 -
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Solvent & Solubility
DMSO : 100 mg/mL (190.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 2.08 mg/mL (3.96 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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.
Purity & Documentation
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Data Sheet (276 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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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[2]. Geron I, et al. Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitors. Cancer Cell. 2008 Apr;13(4):321-30. [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 | 1.9059 mL | 9.5296 mL | 19.0592 mL | 47.6481 mL |
| 5 mM | 0.3812 mL | 1.9059 mL | 3.8118 mL | 9.5296 mL | |
| 10 mM | 0.1906 mL | 0.9530 mL | 1.9059 mL | 4.7648 mL | |
| 15 mM | 0.1271 mL | 0.6353 mL | 1.2706 mL | 3.1765 mL | |
| 20 mM | 0.0953 mL | 0.4765 mL | 0.9530 mL | 2.3824 mL | |
| 25 mM | 0.0762 mL | 0.3812 mL | 0.7624 mL | 1.9059 mL | |
| 30 mM | 0.0635 mL | 0.3177 mL | 0.6353 mL | 1.5883 mL | |
| 40 mM | 0.0476 mL | 0.2382 mL | 0.4765 mL | 1.1912 mL | |
| 50 mM | 0.0381 mL | 0.1906 mL | 0.3812 mL | 0.9530 mL | |
| 60 mM | 0.0318 mL | 0.1588 mL | 0.3177 mL | 0.7941 mL | |
| 80 mM | 0.0238 mL | 0.1191 mL | 0.2382 mL | 0.5956 mL | |
| 100 mM | 0.0191 mL | 0.0953 mL | 0.1906 mL | 0.4765 mL |