DW14383 | FGFR inhibitor | Probechem Biochemicals

Chemical Structure : DW14383

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DW14383 (DW 14383)

货号: PC-21612Not For Human Use, Lab Use Only.

DW14383 is a potent, selective and irreversible inhibitor of FGFR1-4 with IC50 of <0.3 nM, 1.1 nM, <0.3 nM and 0.5 nM for FGFR1/2/3/4 respectively.

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生物&药学活性

DW14383 is a potent, selective and irreversible inhibitor of FGFR1-4 with IC50 of <0.3 nM, 1.1 nM, <0.3 nM and 0.5 nM for FGFR1/2/3/4 respectively.
DW14383 displays >1100-fold selectivity for FGFR1 over recombinant KDR.
DW14383 is more potent than TAS-120 and comparable to AZD4547.
DW14383 (20 nM) completely inhibited FGFR4 phosphorylation and ERK phosphorylation in the Hep3B cells.
DW14383 inhibited the proliferation of FGFR-addicted cells by arresting cells at G1/S phase rather than apoptosis, selectively inhibited the BaF3/TEL-FGFR1 cell proliferation (IC50 < 0.2 nM).
DW14383 (25 mg/kg) effectively inhibited tumor growth in NCI-H1581 and Hep3B subcutaneous xenograft models, significantly suppressed FGFR signaling and inhibited tumor cell proliferation and angiogenesis in FGFR-dependent transplanted tumor tissues.

物理化学性质&存储条件

分子量	498.40
分子式	C22H20BrN5O2S
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	(S)-1-(3-(8-amino-1-(5-bromo-7-methoxybenzo[b]thiophen-2-yl)imidazo[1,5-a]pyrazin-3-yl)pyrrolidin-1-yl)prop-2-en-1-one

参考文献

1. Meng-di Dai, et al. Acta Pharmacol Sin. 2021 Sep;42(9):1498-1506.

DW14383 (DW 14383)

生物&药学活性

物理化学性质&存储条件

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DW14383 (DW 14383)

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