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Chemical Structure : TP-0184
CAS No.: 1628870-27-8
Catalog No.: PC-21414Not For Human Use, Lab Use Only.
Itacnosertib (TP-0184) is a novel potent, selective inhibitor of type I bone morphogenetic protein (BMP) receptor ACVR1 (activin A receptor-type 1, ALK2) and FLT3 with IC50 of 8.0 nM (ALK2).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $198 | In stock | |
| 10 mg | $288 | In stock | |
| 25 mg | $458 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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Itacnosertib (TP-0184) is a novel potent, selective inhibitor of type I bone morphogenetic protein (BMP) receptor ACVR1 (activin A receptor-type 1, ALK2) and FLT3 with IC50 of 8.0 nM (ALK2).
TP-0184 binds to both ACVR1 and FLT3 with high affinity and inhibits FLT3/ACVR1 downstream signaling.
TP-0184 selectively caused growth arrest in FLT3-mutated AML cell lines.
Treatment with TP-0184 or in combination with BCL2 inhibitor, venetoclax dramatically inhibited leukemia growth in FLT3-mutated AML cell lines and patient-derived xenograft models in a dose-dependent manner.
| M.Wt | 468.57 | |
| Formula | C26H28N8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N4-([2,2'-bipyridin]-3-yl)-N2-(3-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidine-2,4-diamine |
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1. Anudishi Tyagi, et al. Leukemia. 2023 Nov 25. doi: 10.1038/s41375-023-02086-6.
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