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Itacnosertib

🥰Excellent
Catalog No. T39104Cas No. 1628870-27-8
Alias TP-0184, TP0184

Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells overexpressing ALK-2, overcomes FLT3 inhibitor resistance and synergistically inhibits AML growth with venetoclax, and possesses potential antitumor and antileukemic activity.

Itacnosertib

Itacnosertib

🥰Excellent
Catalog No. T39104Alias TP-0184, TP0184Cas No. 1628870-27-8
Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells overexpressing ALK-2, overcomes FLT3 inhibitor resistance and synergistically inhibits AML growth with venetoclax, and possesses potential antitumor and antileukemic activity.
Pack SizePriceAvailabilityQuantity
1 mg$119 In Stock
5 mg$293 In Stock
10 mg$436 In Stock
25 mg$719 In Stock
50 mg$987 In Stock
100 mg$1,370 In Stock
200 mg$1,850 In Stock
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Product Introduction

Bioactivity
Description
Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells overexpressing ALK-2, overcomes FLT3 inhibitor resistance and synergistically inhibits AML growth with venetoclax, and possesses potential antitumor and antileukemic activity.
Targets&IC50
Cell proliferation in FLT3-ITD mutant AML cell lines via FLT3/ACVR1 inhibition:< 25  nM
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[1].
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[1].
AliasTP-0184, TP0184
Chemical Properties
Molecular Weight468.55
FormulaC26H28N8O
Cas No.1628870-27-8
SmilesN=1C=CC(=NC1NC2=CC=C(C(OC)=C2)N3CCN(C)CC3)NC=4C=CC=NC4C5=NC=CC=C5
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 10.00 mg/mL (21.34 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1342 mL10.6712 mL21.3424 mL106.7122 mL
5 mM0.4268 mL2.1342 mL4.2685 mL21.3424 mL
10 mM0.2134 mL1.0671 mL2.1342 mL10.6712 mL
20 mM0.1067 mL0.5336 mL1.0671 mL5.3356 mL

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