Vargatef, Free Base (Nintedanib)

Blue Ice

539, 62

Supplied as a powder.

Vargatef is an indolinone derivative that potently inhibits vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR) and fibroblast growth factor receptor (FGFR) kinase activity in enzymatic assays (table 1). It blocks mitogen-activated protein kinase and Akt signaling pathways in three cell types contributing to angiogenesis, namely endothelial cells, pericytes, and smooth muscle cells, and it inhibits cell proliferation with an EC50 of 10-80nM.

Synonyms:
CS-76; BIBF-1120; Trinidad Neeb; Vargatef BIBF; Nintedanib; 1H-Indole-6-carboxylic acid, 2, 3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-, methyl ester; Methyl 3-{[(4-{methyl[(4-methyl-1-piperazinyl)acetyl]amino}phenyl)amino](phenyl)methylene}-2-oxo-6-indolinecarboxylate

CAS No:
656247-17-5

Molecular Formula:
C31H33N5O4

Molecular Weight:
539.62

Purity:
≥99% (HPLC, TLC)

Appearance:
Yellow powder

Solubility:
Soluble in DMSO at 25mg/ml with warming; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.

Elemental Analysis:
Calculated: %C: 68.09, %H: 6.23, %N: 12.81

Storage and Stability:
May be stored at RT for short-term only. Long-term storage is recommended at -20°C. Stable for 12 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap.