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Itacnosertib

SKU: orb1691566

Description

Itacnosertib (TP-0184) is an orally bioavailable small molecule inhibitor targeting ACRV1 (ALK-2), FLT3, and JAK2. It demonstrates antitumor activity by overcoming FLT3 inhibitor resistance and synergizing with venetoclax in AML models, as shown in preclinical in vitro and in vivo studies.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

Key Properties

CAS Number1628870-27-8
MW468.55
Purity99.38% (May vary between batches)
FormulaC26H28N8O
SMILESN=1C=CC(=NC1NC2=CC=C(C(OC)=C2)N3CCN(C)CC3)NC=4C=CC=NC4C5=NC=CC=C5
TargetTGF-beta/Smad,Akt,JAK,mTOR,STAT,PI3K,ALK,FLT
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.13 mM);DMSO:10 mg/mL (21.34 mM)

Bioactivity

Target IC50
Cell proliferation (FLT3-ITD mutant AML cells via FLT3/ACVR1 inhibition):< 25  nM
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.
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.

Storage & Handling

Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Itacnosertib, TP 0184, TP0184, TP-0184

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Key Properties

No computed properties available.

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Itacnosertib (orb1691566)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 1,690.00
5 mg
¥ 3,380.00
1 ml x 10 mM (in DMSO)
¥ 3,640.00
10 mg
¥ 5,070.00
25 mg
¥ 9,230.00
50 mg
¥ 13,390.00
100 mg
¥ 18,330.00
200 mg
¥ 24,570.00
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