Motesanib (Diphosphate)

• Description:

  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 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.

• CAS Number:

  857876-30-3