Motesanib (Diphosphate)

Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.

Product Specifications

CAS Number

[857876-30-3]

Product Name Alternative

AMG 706 (Diphosphate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

C-Kit; VEGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Motesanib-Diphosphate.html

Purity

99.86

Solubility

DMSO : ≥ 110 mg/mL|H2O : 5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC(NCC4(C)C)=C4C=C3.O=P(O)(O)O.O=P(O)(O)O

Molecular Formula

C22H29N5O9P2

Molecular Weight

569.44

Precautions

H302, H315, H319, H335

References & Citations

[1]Polverino A, et al. AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer Res. 2006 Sep 1;66 (17) :8715-21.|[2]Kruser TJ, et al. Augmentation of radiation response by motesanib, a multikinase inhibitor that targets vascular endothelial growth factor receptors. Clin Cancer Res, 2010, 16 (14), 3639-3647.|[3]Coxon A, et al. Broad antitumor activity in breast cancer xenografts by motesanib, a highly selective, oral inhibitor of vascular endothelial growth factor, platelet-derived growth factor, and Kit receptors. Clin Cancer Res, 2009, 15 (1), 110-118.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4

Citation 01

Oncotarget. 2016 Sep 27;7 (39) :63839-63855.|Cell Physiol Biochem. 2018;48 (1) :227-236. |Harvard Medical School LINCS LIBRARY|J Cell Biochem. 2020 Mar;121 (3) :2343-2353.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.