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Itacnosertib

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

🥰Excellent

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

🥰Excellent

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%

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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: 10.00 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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