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

Name: Fedratinib hydrochloride hydrate
Brand: MedChemExpress
SKU: HY-10409A
Rating: 5.0 (51 reviews)

Art. -Nr.: HY-10409A Reinheit: 99.92%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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CAS. Nr. : 1374744-69-0

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Kostenlose Probe (0.1 - 0.2 mg)	Jetzt bewerben
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
200 mg	Auf Lager	Estimated Time of Arrival: December 31
500 mg	Auf Lager	Estimated Time of Arrival: December 31
1 g	Auf Lager	Estimated Time of Arrival: December 31
2 g	Auf Lager	Estimated Time of Arrival: December 31
5 g	Auf Lager	Estimated Time of Arrival: December 31
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Based on 51 publication(s) in Google Scholar

Other Forms of Fedratinib hydrochloride hydrate:

Fedratinib In-stock
Fedratinib-d₉ Angebot einholen
Fedratinib hydrochloride hydrate (Standard) Angebot einholen

51 Publications Citing Use of MCE Fedratinib hydrochloride hydrate

Cell Proliferation/Viability Assay

: 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.

: 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.

: 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.

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle JAK Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

JAK1 JAK2 JAK3 Tyk2 JAK

Biologische Aktivität
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

IC₅₀ & Target^[1]

JAK2

3 nM (IC₅₀)

JAK2(V617F)

3 nM (IC₅₀)

Flt3

15 nM (IC₅₀)

Ret

48 nM (IC₅₀)

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.

Molekulargewicht

615.62

Formel

C₂₇H₄₀Cl₂N₆O₄S

CAS. Nr.

1374744-69-0

Appearance

Solid

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

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

4°C, sealed storage, away from moisture

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

Lösungsmittel & Löslichkeit

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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 (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.

Molaritätsrechner
Verdünnungsrechner

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: 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).

Reinheit & Dokumentation

Purity: 99.92%

Select Batch:

Data Sheet (278 KB) SDS (394 KB)

COA (253 KB) HNMR (321 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

Verweise

[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

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.

Fedratinib hydrochloride hydrate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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

Kundenbewertung

Other Forms of Fedratinib hydrochloride hydrate:

Fedratinib hydrochloride hydrate Related Antibodies

51 Publications Citing Use of MCE Fedratinib hydrochloride hydrate

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle JAK Isoform-spezifische Produkte anzeigen:

Biologische Aktivität

Reinheit & Dokumentation

Verweise

Kundenbewertung

Fedratinib hydrochloride hydrate Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Fedratinib hydrochloride hydrate Related Classifications

Keywords:

Ihre kürzlich angesehenen Produkte:

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