Sigma-Aldrich Motesanib, Diphosphate - C

Assay

≥98% (HPLC)

Quality Level

100

Form

solid

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
desiccated (hygroscopic)
protect from light

Color

off-white

Solubility

DMSO: 50 mg/mL

Storage Temp.

−20°C

Inchi

1S/C22H23N5O.2H3O4P/c1-22(2)14-26-19-12-16(5-6-18(19)22)27-21(28)17-4-3-9-24-20(17)25-13-15-7-10-23-11-8-15;2*1-5(2,3)4/h3-12,26H,13-14H2,1-2H3,(H,24,25)(H,27,28);2*(H3,1,2,3,4)

Inchi Key

ONDPWWDPQDCQNJ-UHFFFAOYSA-N

Related Categories

Phosphates

General Description

A cell-permeable, bioavailable nicotinamide derivative that acts as a highly potent, ATP-competitive multi-kinase inhibitor (IC₅₀= 2, 3, 6, 8 nM for VEGFR1, VEGFR2, VEGFR3, and Kit, respectively). Also inhibits the activity of PDGFR and RET kinases, albeit at higher concentrations (IC₅₀= 84 and 39 nM, respectively). Does not affect the activities of EGFR, Src, and p38 kinases (IC₅₀>3 µM) and 47 other protein kinases. Inhibits VEGF-induced (IC₅₀= 10 nM), but not bFGF-induced (IC₅₀>3 µM) proliferation of HUVECs. Also shown to diminish VEGF-induced angiogenesis in a rat corneal model (ED₅₀= 2.1 mg/kg, b.i.d; p.o.) and suppresses the growth of A431 human epidermoid xenografts in mice (10 to 100 mg/kg, b.i.d). Displays desirable pharmacokinetic properties (t = 6.7 h; C_max= 787 ng/ml).A cell-permeable, bioavailable nicotinamide derivative that acts as a highly potent, ATP-competitive multi-kinase inhibitor (IC₅₀= 2, 3, 6, 8 nM for VEGFR1, VEGFR2, VEGFR3, and Kit, respectively). Also inhibits the activity of PDGFR and RET kinases, albeit at higher concentrations (IC₅₀= 84 and 39 nM, respectively). Does not affect the activities of EGFR, Src, and p38 kinases (IC₅₀>3 µM) and 47 other protein kinases. Inhibits VEGF-induced (IC₅₀= 10 nM), but not bFGF-induced (IC₅₀>3 µM) proliferation of HUVECs. Also shown to diminish VEGF-induced angiogenesis in a rat corneal model (ED₅₀= 2.1 mg/kg, b.i.d; p.o.) and suppresses the growth of A431 human epidermoid xenografts in mice (10 to 100 mg/kg, b.i.d). Displays desirable pharmacokinetic properties (t = 6.7 h; C_max= 787 ng/ml).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Biochem/Physiol Actions

Cell permeable: yesPrimary Target
VEGFRReversible: yesTarget IC₅₀: 2 nM, 3 nM, 6 nM, 6 nM, 8 nM for VEGFR1, VEGFR2, Flk-1, VEGFR3, and KIT respecitively

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Wang, Y., et al. 2014.Biochem. Pharmacol. 90,367.

Benjamin, R., et al. 2011.Cancer Chemother. Pharmacol. 68,69.

Li, C., et al. 2009.Drug Metab. Dispos. 37,1378.

Sherman, S., et al. 2008.N. Engl. J. Med. 359,31.

Polverino, A., et al. 2006.Cancer Res. 66,8715.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany