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HM43239

Name: HM43239
Brand: TargetMol
SKU: T9428
Price: 45 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9428Cas No. 2294874-49-8

Alias Tuspetinib, 2569527-64-4

HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1/2 and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells [1] [2] [3].

HM43239

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Purity: 99.7%

Catalog No. T9428Alias Tuspetinib, 2569527-64-4Cas No. 2294874-49-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$45	In Stock	In Stock
5 mg	$106	In Stock	In Stock
10 mg	$169	In Stock	In Stock
25 mg	$343	In Stock	In Stock
50 mg	$515	In Stock	In Stock
100 mg	$718	In Stock	In Stock
200 mg	$950	-	In Stock
1 mL x 10 mM (in DMSO)	$117	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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Purity:99.7%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1/2 and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells [1] [2] [3].
Targets&IC50	FLT3 (D835Y):1.0 nM, FLT3 (WT):1.1 nM, FLT3 (ITD):1.8 nM
In vitro	HM43239 potently inhibits the growth of acute myeloid leukemia cell lines harboring FLT3 ITD mutation like MV4-11 (IC 50 : 1.3 nM), MOLM-13 (IC 50 : 5.1 nM), and MOLM-14 (IC 50 : 2.9 nM). Besides, HM43239 inhibits KG1a cells (CD34+/CD38- cells) proliferation [1]. HM43239 induces the caspase 3/7-dependent apoptosis of leukemic stem cell (LSC) marker-expressing KG1a cells (CD34+/CD38- cells) [1]. HM43239 potently inhibits phosphorylation of SYK, STAT3, and STAT5 in KG1a cells [3].
In vivo	HM43239 exhibits the excellent dose proportional antitumor activity in mouse models xenografted with both MV4-11 and MOLM-13 cell lines without any significant toxicity [1]. HM43239 prolongs survival in FLT3 ITD/TKD double mutated xenograft mouse models [3].
Synonyms	Tuspetinib, 2569527-64-4

Chemical Properties

Molecular Weight	501.07
Formula	C₂₉H₃₃ClN₆
Cas No.	2294874-49-8
Smiles	C[C@H]1CN(Cc2cc(Nc3ncc(Cl)c(n3)-c3c[nH]c4cc(C)ccc34)cc(c2)C2CC2)C[C@@H](C)N1
Relative Density.	1.258 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (498.93 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2.5 mg/mL (4.99 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	1.9957 mL	9.9786 mL	19.9573 mL	99.7865 mL
5 mM	0.3991 mL	1.9957 mL	3.9915 mL	19.9573 mL
10 mM	0.1996 mL	0.9979 mL	1.9957 mL	9.9786 mL
20 mM	0.0998 mL	0.4989 mL	0.9979 mL	4.9893 mL
50 mM	0.0399 mL	0.1996 mL	0.3991 mL	1.9957 mL
100 mM	0.0200 mL	0.0998 mL	0.1996 mL	0.9979 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