Cat. No.: HY-109179A

Itacnosertib hydrochloride

(Synonyms: TP-0184 hydrochloride)

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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.

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Pureté: 99.43%
CAS No.: 2409543-84-4
Formule: C₂₆H₂₉ClN₈O
Masse moléculaire:505.01

Stockage:

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

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

Activité biologique

Description

IC₅₀ & Target^[2]

ACVR1

8 nM (IC₅₀)

JAK2

8540 nM (IC₅₀)

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Smad1
Smad3

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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.

Essai clinique

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

Chemical Information

CAS No. 2409543-84-4
Appearance Solid
Masse moléculaire 505.01
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

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

Solvant et solubilité

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.

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)

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)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (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)
Instruction de manipulation (2659 KB)

Références

[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

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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 hydrochloride Related Classifications