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Derazantinib

Chemical Structure : Derazantinib

CAS No.: 1234356-69-4

Derazantinib (ARQ-087;ARQ087)

Catalog No.: PC-60038Not For Human Use, Lab Use Only.

Derazantinib (ARQ-087) is a novel potent, ATP competitive multi-kinase inhibitor with IC50 of FGFR1/2/3 with IC50 of 1.8-4.5 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Derazantinib (ARQ-087) is a novel potent, ATP competitive multi-kinase inhibitor with IC50 of FGFR1/2/3 with IC50 of 1.8-4.5 nM.
Derazantinib (ARQ-087) also inhibits FGFR4, Src, Abl, RET, etc. (IC50<50 nM).
Derazantinib (ARQ-087) inhibits FGFR2 auto-phosphorylation and other proteins downstream in the FGFR pathway (FRS2α, AKT, ERK), shows potent anti-proliferative effect in cell lines driven by FGFR dysregulation.
Derazantinib (ARQ-087) shows tumor growth inhibition in vivo in xenograft tumor models.

Physicochemical Properties

M.Wt 468.576
Formula C29H29FN4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(6R)-6-(2-fluorophenyl)-N-(3-{2-[(2-methoxyethyl)amino]ethyl}phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine

References

1. Hall TG, et al. PLoS One. 2016 Sep 14;11(9):e0162594.

2. Yu Y, et al. Anticancer Drugs. 2017 Jun;28(5):503-513.

3. Balek L, et al. Bone. 2017 Dec;105:57-66.

4. Papadopoulos KP, et al. Br J Cancer. 2017 Nov 21;117(11):1592-1599.

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