Cat. No.: HY-109179

Itacnosertib

(Synonyms: TP-0184)

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Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC₅₀=8 nM) and JAK2 (IC₅₀=8540 nM). Itacnosertib exhibits anti-leukemic activity.

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Pureté: 99.06%
CAS No.: 1628870-27-8
Formule: C₂₆H₂₈N₈O
Masse moléculaire:468.55

Stockage:

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

Itacnosertib Chemical Structure

CAS No.: 1628870-27-8

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC₅₀=8 nM) and JAK2 (IC₅₀=8540 nM). Itacnosertib exhibits anti-leukemic activity^[1]^[2].

IC₅₀ & Target^[1]

ACVR1

8 nM (IC₅₀)

JAK2

8540 nM (IC₅₀)

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Smad1
Smad3

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In Vitro

Itacnosertib (0-200 nM, 24-48 h) arrests the cell cycle of MOLM-13, MOLM-14 and MV4-11 at G1/G0 phase, inhibits the proliferation of acute myeloid leukemia (AML) cells, IC₅₀s for MOLM-13, MOLM-14 and MV4-11 (FLT3-mutated AML cells) are 6.4, 1.2 and 1.3 nM, respectively. Itacnosertib inhibits the AML FLT3-wildtype cell with IC₅₀ > 100 nM^[2].
Itacnosertib inhibits the activation of FLT3 and ACVR1 downstream signaling pathways, inhibits serine biosynthesis and amino acid transport pathways^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[2]

Cell Line:

MOLM-13, MOLM-14 and MV4-11
Concentration:

0-1000 nM
Incubation Time:

24-48 h
Result:

Inhibited the phosphorylation of STAT5, MKK3, ERK, PI3K, AKT, mTOR, p-4E-BP1, p-S6K and SMAD1/5.

Cell Cycle Analysis^[2]

Cell Line:

MOLM-13, MOLM-14 and MV4-11
Concentration:

0-200 nM
Incubation Time:

24-48 h
Result:

Arrested the cell cycle at subG1 phase.

In Vivo

Itacnosertib (50-200 mg/kg, po, once weekly for 5-6 weeks) exhibits antitumor activity against MOLM-13 in mouse models^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Mouse MOLM-13 xenograft models^[2]
Dosage:

50-200 mg/kg
Administration:

po, once weekly for 5-6 weeks
Result:

Inhibited the leukemia growth, prolonged the mice survival.

Chemical Information

CAS No. 1628870-27-8
Appearance Solid
Masse moléculaire 468.55
Formule C₂₆H₂₈N₈O
Color Off-white to gray
SMILES

CN1CCN(C2=CC=C(NC3=NC=CC(NC4=CC=CN=C4C5=NC=CC=C5)=N3)C=C2OC)CC1
Synonyms

TP-0184
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 12.5 mg/mL (26.68 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1342 mL

10.6712 mL

21.3424 mL

5 mM

0.4268 mL

2.1342 mL

4.2685 mL

10 mM

0.2134 mL

1.0671 mL

2.1342 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 1.25 mg/mL (2.67 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.25 mg/mL (2.67 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.25 mg/mL (2.67 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (252 KB)
- English - EN (252 KB)
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- Español - ES (252 KB)
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- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Mollard, Alexis; Warner, Steven L.; Flynn, Gary A.; Vankayalapati, Hariprasad; Bearss, David J. Preparation of [(piperazinylphenyl)amino]pyrimidine derivatives as JAK2 and ALK2 inhibitors. WO2014151871 A2

[2]. Tyagi A, et al., TP-0184 inhibits FLT3/ACVR1 to overcome FLT3 inhibitor resistance and hinder AML growth synergistically with venetoclax. Leukemia. 2024 Jan;38(1):82-95. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1342 mL	10.6712 mL	21.3424 mL	53.3561 mL
	5 mM	0.4268 mL	2.1342 mL	4.2685 mL	10.6712 mL
	10 mM	0.2134 mL	1.0671 mL	2.1342 mL	5.3356 mL
	15 mM	0.1423 mL	0.7114 mL	1.4228 mL	3.5571 mL
	20 mM	0.1067 mL	0.5336 mL	1.0671 mL	2.6678 mL
	25 mM	0.0854 mL	0.4268 mL	0.8537 mL	2.1342 mL

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Itacnosertib

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform JAK

Voir tous les produits spécifiques à Isoform STAT

Voir tous les produits spécifiques à Isoform PI3K

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform mTOR

Voir tous les produits spécifiques à Isoform TGF-beta/Smad

Voir tous les produits spécifiques à Isoform TGF-β Receptor

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Itacnosertib Related Classifications

HY-109179 Related Classifications