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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 Size | Price | Availability | Quantity |
---|---|---|---|
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 |
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]. |
Alias | TP-0184, TP0184 |
Molecular Weight | 468.55 |
Formula | C26H28N8O |
Cas No. | 1628870-27-8 |
Smiles | N=1C=CC(=NC1NC2=CC=C(C(OC)=C2)N3CCN(C)CC3)NC=4C=CC=NC4C5=NC=CC=C5 |
Storage | store 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
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