Cat. No.: HY-10409A

Fedratinib hydrochloride hydrate

(Synonyms: TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate)

54 Cited Publications

Customer Review

Based on 54 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity: 99.92%
CAS No.: 1374744-69-0
Formula: C₂₇H₄₀Cl₂N₆O₄S
Molecular Weight:615.62

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Fedratinib hydrochloride hydrate Chemical Structure

CAS No.: 1374744-69-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (54)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

JAK2

3 nM (IC₅₀)

JAK2(V617F)

3 nM (IC₅₀)

Flt3

15 nM (IC₅₀)

Ret

48 nM (IC₅₀)

All JAK Isoforms :

In Vitro

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.

In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57Bl/6 mice induced by the JAK2V617F mutation^[1]
Dosage:

60 mg/kg, 120 mg/kg
Administration:

Oral gavage; twice daily; for 42 days
Result:

Showed a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis.

Chemical Information

CAS No. 1374744-69-0
Appearance Solid
Molecular Weight 615.62
Formula C₂₇H₄₀Cl₂N₆O₄S
Color White to yellow
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
Synonyms

TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Publications (54)

All Cell Proliferation/Viability AssayWBIF

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Journal Impact Factor

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

Uridine-derived ribose fuels glucose-restricted pancreatic cancer. [Abstract]

2023 Jun;618(7963):151-158. PMID: 37198494
Science

Antifibrotic drug finerenone restores fertility in premature ovarian insufficiency. [Abstract]

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

Palmitoylation-mediated regulation of KAT2A promotes lung metastasis in breast cancer. [Abstract]

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
Mol Ther Oncol

2024 Jun 07.
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 hydrochloride hydrate 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 hydrochloride hydrate 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.
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

The novel role of activating receptor KIR2DS5 in preeclampsia. [Abstract]

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

The Effects of STRA6 Regulation of the Circadian Rhythm on Choroidal Neovascularization. [Abstract]

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):2071. 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 hydrochloride hydrate 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.
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 hydrochloride hydrate 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.
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
bioRxiv

2025 Nov 26.
University of Pennsylvania

2025.
SSRN

2025 Jul 4.
bioRxiv

2025 February 21.
bioRxiv

2024 September 24.
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
University of Michigan

2024.
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
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
University of Michigan

2023 Sep.
Patent

US20210128545A1.
University of California

2021 Apr.
Research Square Preprint

2020 Jun.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (162.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 100 mg/mL (162.44 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	1.6244 mL	8.1219 mL	16.2438 mL	40.6095 mL
	5 mM	0.3249 mL	1.6244 mL	3.2488 mL	8.1219 mL
	10 mM	0.1624 mL	0.8122 mL	1.6244 mL	4.0609 mL
	15 mM	0.1083 mL	0.5415 mL	1.0829 mL	2.7073 mL
	20 mM	0.0812 mL	0.4061 mL	0.8122 mL	2.0305 mL
	25 mM	0.0650 mL	0.3249 mL	0.6498 mL	1.6244 mL
	30 mM	0.0541 mL	0.2707 mL	0.5415 mL	1.3536 mL
	40 mM	0.0406 mL	0.2030 mL	0.4061 mL	1.0152 mL
	50 mM	0.0325 mL	0.1624 mL	0.3249 mL	0.8122 mL
	60 mM	0.0271 mL	0.1354 mL	0.2707 mL	0.6768 mL
	80 mM	0.0203 mL	0.1015 mL	0.2030 mL	0.5076 mL
	100 mM	0.0162 mL	0.0812 mL	0.1624 mL	0.4061 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Fedratinib hydrochloride hydrate

54 Cited Publications

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Fedratinib hydrochloride hydrate

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

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Publications Citing Use of MedChemExpress (MCE) Fedratinib hydrochloride hydrate

All JAK Isoforms

Biological Activity

Chemical Information

Publications (54)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Fedratinib hydrochloride hydrate Related Classifications

HY-10409A Related Classifications