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Itacnosertib

Name: Itacnosertib
Brand: TargetMol
SKU: T39104
Price: 88 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T39104Cas No. 1628870-27-8

Alias TP-0184, TP0184

Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells overexpressing ALK-2, overcomes FLT3 inhibitor resistance and synergistically inhibits AML growth with venetoclax, and possesses potential antitumor and antileukemic activity.

Itacnosertib

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Purity: 99.38%

Catalog No. T39104Alias TP-0184, TP0184Cas No. 1628870-27-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$88	In Stock	In Stock
5 mg	$213	In Stock	In Stock
10 mg	$347	In Stock	In Stock
25 mg	$662	In Stock	In Stock
50 mg	$987	In Stock	In Stock
100 mg	$1,370	In Stock	In Stock
200 mg	$1,850	-	In Stock
1 mL x 10 mM (in DMSO)	$235	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.38%

Appearance:Solid

Color:Gray

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells overexpressing ALK-2, overcomes FLT3 inhibitor resistance and synergistically inhibits AML growth with venetoclax, and possesses potential antitumor and antileukemic activity.
Targets&IC50	Cell proliferation (FLT3-ITD mutant AML cells via FLT3/ACVR1 inhibition):< 25  nM
In vitro	Itacnosertib is a dual FLT3/ACVR1 inhibitor. Itacnosertib was tested on AML cell lines harboring FLT3-ITD mutations (MV4-11, MOLM-13, MOLM-14), showing potent inhibition of cell proliferation (IC₅₀ < 25 nM) and downregulation of FLT3- and ACVR1-mediated signaling (e.g., p-FLT3, p-STAT5, p-AKT, p-SMAD1/5). Itacnosertib also induced G0/G1 cell cycle arrest and inhibited serine biosynthesis and amino acid transport genes in FLT3-mutant AML cells[1].
In vivo	In NSG mice xenografted with FLT3-ITD AML cells, oral administration of Itacnosertib (50–200 mg/kg, 3×/week) significantly reduced leukemia burden and prolonged survival (median survival increased from 18 to 32 days). In patient-derived xenograft (PDX) models, Itacnosertib at 200 mg/kg extended survival from 100 to 183 days[1].
Synonyms	TP-0184, TP0184

Chemical Properties

Molecular Weight	468.55
Formula	C₂₆H₂₈N₈O
Cas No.	1628870-27-8
Smiles	N=1C=CC(=NC1NC2=CC=C(C(OC)=C2)N3CCN(C)CC3)NC=4C=CC=NC4C5=NC=CC=C5

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 10 mg/mL (21.34 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.13 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1342 mL	10.6712 mL	21.3424 mL	106.7122 mL
5 mM	0.4268 mL	2.1342 mL	4.2685 mL	21.3424 mL
10 mM	0.2134 mL	1.0671 mL	2.1342 mL	10.6712 mL
20 mM	0.1067 mL	0.5336 mL	1.0671 mL	5.3356 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc