Clifutinib | FLT3-ITD inhibitor | Probechem Biochemicals

Chemical Structure : Clifutinib

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Clifutinib (HEC-73543, HEC73543)

货号: PC-24405Not For Human Use, Lab Use Only.

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生物&药学活性

Clifutinib (HEC73543) is potent, selective FLT3-ITD (internal tandem duplication mutations of FLT3) inhibitor with biochemical IC50 of 15.1 nM, exhibits significant antiproliferative activity against Ba/F3-FLT3-ITD cells with IC50 of 0.9 nM.
Clifutinib potently suppresses proliferation of MV-4-11 and MOLM-13 AML cells harboring FLT3-ITD with IC50 of 1.5 and 1.4 nM, respectively.
Clifutinib only exhibits >80% inhibition against 12 out of 414 kinases at 1 uM,, does not inhibit KIT kinase (IC50 = 1790 nM).
Clifutinib shows minimal or no antiproliferative effects were observed against FLT3-ITD-negative cell lines such as RS4;11, HL-60, MOLT-4, RPMI8226, and K562.
Clifutinib demonstrates significant antiproliferative activity against BaF3 cells driven by the most common FLT3-TKD mutations (D835Y, D835H, and D835V), with IC50 values of 5.4, 10.9, and 37.4 nM, respectively.
Clifutinib exhibits favorable antiproliferative activity against FLT3-ITD mutant leukemia cells but not against FLT3 wild-type cells.
Clifutinib induces apoptosis in FLT3-ITD mutant AML cells, inhibits the phosphorylation of FLT3, ERK, AKT, and STAT5 in a dose-dependent manner without affecting their total protein levels.
Clifutinib (1.5 or 4.5 mg/kg, orally once daily) exhibited rapid and near-complete tumor regression, with no tumor rebound observed during the 31-day post-treatment period in MV-4-11 and MOLM-13 xenograft tumor models.

物理化学性质&存储条件

分子量	502.62
分子式	C29H34N4O4
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-(5-(tert-Butyl)isoxazol-3-yl)-3-(4-((4-(3-morpholinopropoxy)phenyl)ethynyl)phenyl)urea

参考文献

1. Liu B, et al. J Med Chem. 2025 Apr 11. doi: 10.1021/acs.jmedchem.4c03023.

2. Cliff Cheng, et al. Cancer Res (2017) 77 (13_Supplement): 2093.

Clifutinib (HEC-73543, HEC73543)

生物&药学活性

物理化学性质&存储条件

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Clifutinib (HEC-73543, HEC73543)

生物&药学活性

物理化学性质&存储条件

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