Fedratinib (Synonyms: TG-101348; SAR 302503)

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

製品番号: HY-10409 純度: 99.83%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 936091-26-8

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 63	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 63	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$55	在庫あり	Estimated Time of Arrival: December 31
10 mg	$77	在庫あり	Estimated Time of Arrival: December 31
50 mg	$140	在庫あり	Estimated Time of Arrival: December 31
100 mg	$165	在庫あり	Estimated Time of Arrival: December 31
200 mg	$275	在庫あり	Estimated Time of Arrival: December 31
500 mg	$605	在庫あり	Estimated Time of Arrival: December 31
1 g	$1045	在庫あり	Estimated Time of Arrival: December 31
2 g	$1815	在庫あり	Estimated Time of Arrival: December 31
5 g	$3575	在庫あり	Estimated Time of Arrival: December 31
10 g		お問い合わせ
50 g		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 51 publication(s) in Google Scholar

Other Forms of Fedratinib:

Fedratinib hydrochloride hydrate 在庫あり
Fedratinib-d₉ お問い合わせ
Fedratinib (Standard) お問い合わせ

顧客検証

Cell Proliferation/Viability Assay

: 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.

: 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.

: 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.

JAK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

JAK1 JAK2 JAK3 Tyk2 JAK

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

JAK2

3 nM (IC₅₀)

JAK2(V617F)

3 nM (IC₅₀)

Flt3

15 nM (IC₅₀)

Ret

48 nM (IC₅₀)

Cellular Effect

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]
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]
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]
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]

体外実験

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.

体内実験

Fedratinib (TG101348; 60-120 mg/kg; oral gavage; twice daily; for 42 days; C57Bl/6 mice) 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.

臨床実験

分子量

524.68

分子式

C₂₇H₃₆N₆O₃S

CAS 番号

936091-26-8

Appearance

Solid

Color

White to light yellow

SMILES

O=S(C1=CC=CC(NC2=NC(NC3=CC=C(C=C3)OCCN4CCCC4)=NC=C2C)=C1)(NC(C)(C)C)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9059 mL	9.5296 mL	19.0592 mL
5 mM	0.3812 mL	1.9059 mL	3.8118 mL
10 mM	0.1906 mL	0.9530 mL	1.9059 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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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: ≥ 2.08 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

純度とドキュメンテーション

純度: 99.87%

Select Batch:

データシート (276 KB) SDS (393 KB)

COA (250 KB) HNMR (281 KB) LCMS (266 KB)

取扱説明書 (2659 KB)

参考文献

[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	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

Fedratinib Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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 (Synonyms: TG-101348; SAR 302503)

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Other Forms of Fedratinib:

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JAK アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Fedratinib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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Fedratinib (Synonyms: TG-101348; SAR 302503)

カスタマーレビュー

Other Forms of Fedratinib:

Fedratinib 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

JAK アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Fedratinib 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Fedratinib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

Request for HNMR Report

Request for HNMR Report