Danatinib

Chemical Structure : Danatinib

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货号: PC-23629Not 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	461.83
分子式	C21H15ClF3N5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-(4-(3-amino-6-methylisoxazolo[3,4-b]pyridin-4-yl)phenyl)-3-(4-chloro-3-(trifluoromethyl)phenyl)urea

参考文献

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.

Danatinib

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