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Chemical Structure| 857876-30-3 Chemical Structure| 857876-30-3

Structure of Motesanib Diphosphate
CAS No.: 857876-30-3

Chemical Structure| 857876-30-3

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Motesanib diphosphate is ATP-competitive inhibitor of VEGFR1, VEGFR2 and VEGFR3 with IC50 of 2 nM, 3 nM and 6 nM, respectively. It also shows better inhibitory activity against c-Kit, PDGFR, and RET.

Synonyms: AMG 706 Diphosphate; AMG 706; Motesanib

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Product Details of Motesanib Diphosphate

CAS No. :857876-30-3
Formula : C22H29N5O9P2
M.W : 569.44
SMILES Code : O=C(NC1=CC2=C(C(C)(CN2)C)C=C1)C3=CC=CN=C3NCC4=CC=NC=C4.O=P(O)(O)O.O=P(O)(O)O
Synonyms :
AMG 706 Diphosphate; AMG 706; Motesanib
MDL No. :MFCD12407403
InChI Key :ONDPWWDPQDCQNJ-UHFFFAOYSA-N
Pubchem ID :16097729

Safety of Motesanib Diphosphate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Motesanib Diphosphate

RTK

Isoform Comparison

Biological Activity

Target
  • VEGFR1

    VEGFR1, IC50:2 nM

  • VEGFR3

    VEGFR3, IC50:6 nM

  • VEGFR2

    VEGFR2/Flk1, IC50:3 nM

    VEGFR2, IC50:3 nM

  • PDGFR

    PDGFR, IC50:84 nM

  • c-Kit

    Kit, IC50:8 nM

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.78mL

1.76mL

0.88mL

17.56mL

3.51mL

1.76mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

[1]Kruser TJ, Wheeler DL, et al. Augmentation of radiation response by motesanib, a multikinase inhibitor that targets vascular endothelial growth factor receptors. Clin Cancer Res. 2010 Jul 15;16(14):3639-47.

[2]Polverino A, Coxon 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.

[3]Polverino A, Coxon A, Starnes C, Diaz Z, DeMelfi T, Wang L, Bready J, Estrada J, Cattley R, Kaufman S, Chen D, Gan Y, Kumar G, Meyer J, Neervannan S, Alva G, Talvenheimo J, Montestruque S, Tasker A, Patel V, Radinsky R, Kendall R. 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

[4]Kruser TJ, Wheeler DL, Armstrong EA, Iida M, Kozak KR, van der Kogel AJ, Bussink J, Coxon A, Polverino A, Harari PM. Augmentation of radiation response by motesanib, a multikinase inhibitor that targets vascular endothelial growth factor receptors. Clin Cancer Res. 2010 Jul 15;16(14):3639-47

[5]Coxon A, Bush T, Saffran D, Kaufman S, Belmontes B, Rex K, Hughes P, Caenepeel S, Rottman JB, Tasker A, Patel V, Kendall R, Radinsky R, Polverino A. 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 Jan 1;15(1):110-8

[6]Sherman SI, Wirth LJ, Droz JP, Hofmann M, Bastholt L, Martins RG, Licitra L, Eschenberg MJ, Sun YN, Juan T, Stepan DE, Schlumberger MJ; Motesanib Thyroid Cancer Study Group. Motesanib diphosphate in progressive differentiated thyroid cancer. N Engl J Med. 2008 Jul 3;359(1):31-42

 

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