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Chemical Structure : Danatinib
Catalog No.: PC-21415Not For Human Use, Lab Use Only.
Danatinib is a potent and selective FLT3 inhibitor with IC50 of 3 nM, overcomes acquired resistance and shows effective inhibition against FLT3-ITD and/or FLT3-TKD mutations.
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Danatinib is a potent and selective FLT3 inhibitor with IC50 of 3 nM, overcomes acquired resistance and shows effective inhibition against FLT3-ITD and/or FLT3-TKD mutations.
Danatinib exhibits excellent selectivity profile on 310 kinases with an S score (1) of 0.058, with exception kinases RET and KIT (IC50<10 nM).
Danatinib displays antiproliferative activities by targeting FLT3-ITD and/or secondary mutations, which include FLT3-ITD-N676D, FLT3-ITD-F691L, FLT3-ITD-G697R, FLT3-ITD-D835V, FLT3-ITD-D835Y and FLT3-ITD-Y842H (IC50=0.9-818 nM).
Danatinib has stronger antiproliferative effects compared to linifanib in both MV4-11 and MOLM-13 cells with IC50 of 4.6 nM and 0.89 nM, respectively.
Danatinib effectively induces G0-G1 cell cycle arrest in both MV4-11 and MOLM-13 cells and triggers cell death via inhibition of FLT3-mediated signaling.
Danatinib dose-dependently blocks the phosphorylation of FLT3 and completely suppresses FLT3 autophosphorylation at 100 nM in MV4–11 cells.
Danatinib dose-dependently inhibits the phosphorylation of FLT3 and its downstream signaling pathway mediators STAT5, AKT and ERK, decreasse the cellular ROS level in FLT3-ITD AML cells.
Danatinib (10 -50 mg/kg, once a day, i.p.) exhibit excellent antitumor efficacy in AML MV4–11 xenograft model, without myelosuppressive toxicity.
| M.Wt | 461.83 | |
| Formula | C21H15ClF3N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Z.H. Shi, et al.Bioorg. Med. Chem., 26 (16) (2018), pp. 4735-4744
2. Shan-Liang Sun, et al. Biomed Pharmacother. 2023 Nov 23:169:115905.
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