Cat. No.: HY-109179A

Itacnosertib hydrochloride

(Synonyms: TP-0184 hydrochloride)

Customer Review

Based on 1 Customer Validation

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

For research use only. We do not sell to patients.

Purity: 99.43%
CAS No.: 2409543-84-4
Formula: C₂₆H₂₉ClN₈O
Molecular Weight:505.01

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Itacnosertib hydrochloride Chemical Structure

CAS No.: 2409543-84-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[2]

ACVR1

8 nM (IC₅₀)

JAK2

8540 nM (IC₅₀)

All JAK Isoforms :

All STAT Isoforms :

All PI3K Isoforms :

All Akt Isoforms :

All mTOR Isoforms :

All TGF-beta/Smad Isoforms :

Smad1
Smad3

All TGF-β Receptor Isoforms :

In Vitro

Itacnosertib hydrochloride (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 hydrochloride inhibits the AML FLT3-wildtype cell with IC₅₀ > 100 nM^[2].
Itacnosertib hydrochloride 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 hydrochloride (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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2409543-84-4
Appearance Solid
Molecular Weight 505.01
Formula C₂₆H₂₉ClN₈O
Color Off-white to light brown
SMILES

CN1CCN(C2=CC=C(NC3=NC=CC(NC4=CC=CN=C4C5=NC=CC=C5)=N3)C=C2OC)CC1.[H]Cl
Synonyms

TP-0184 hydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 5.56 mg/mL (11.01 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

1.9802 mL

9.9008 mL

19.8016 mL

5 mM

0.3960 mL

1.9802 mL

3.9603 mL

10 mM

0.1980 mL

0.9901 mL

1.9802 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- 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)
Handling Instructions (2659 KB)

References

[1]. Mollard A, et al. Preparation of [(piperazinylphenyl)amino]pyrimidine derivatives as JAK2 and ALK2 inhibitors. WO2014151871A2. 2014-09-25.

[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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9802 mL	9.9008 mL	19.8016 mL	49.5040 mL
	5 mM	0.3960 mL	1.9802 mL	3.9603 mL	9.9008 mL
	10 mM	0.1980 mL	0.9901 mL	1.9802 mL	4.9504 mL

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Itacnosertib hydrochloride

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

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Posttranslational Modification Library

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All JAK Isoforms

All STAT Isoforms

All PI3K Isoforms

All Akt Isoforms

All mTOR Isoforms

All TGF-beta/Smad Isoforms

All TGF-β Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Itacnosertib hydrochloride Related Classifications