WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 123214
CAS#: 857876-30-3 (phosphate)
Description: Motesanib, also known as AMG-706, is the orally bioavailable multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. Motesanib selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation.
MedKoo Cat#: 123214
Name: Motesanib phosphate
CAS#: 857876-30-3 (phosphate)
Chemical Formula: C22H29N5O9P2
Exact Mass:
Molecular Weight: 569.4475
Elemental Analysis: C, 46.40; H, 5.13; N, 12.30; O, 25.29; P, 10.88
Related CAS #: 453562-69-1 (free base) 857876-30-3 (phosphate)
Synonym: AMG 706; AMG706; AMG706; motesanib phosphate; motesanib diphosphate;
IUPAC/Chemical Name: N-(3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-2-[(pyridin-4- ylmethyl)amino]pyridine-3-carboxamide diphosphate
InChi Key: DJJCDCBLOWTOJD-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H23N5O.H4O7P2/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;1-8(2,3)7-9(4,5)6/h3-12,26H,13-14H2,1-2H3,(H,24,25)(H,27,28);(H2,1,2,3)(H2,4,5,6)
SMILES Code: O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC4=C(C=C3)C(C)(C)CN4.O=P(O)(OP(O)(O)=O)O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM. |
| In vitro activity: | This study found that motesanib alone exerted antiproliferative, antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. Combination with DUP-697 increased the antiproliferative, antiangiogenic and apoptotic effects. Reference: Asian Pac J Cancer Prev. 2016;17(3):1103-10. https://pubmed.ncbi.nlm.nih.gov/27039732/ |
| In vivo activity: | Across all three mouse xenograft models, motesanib treatment resulted in significant dose-dependent reductions in tumor growth, compared with vehicle-treated controls, and in marked reductions in viable tumor fraction and blood vessel density. There was a significantly greater reduction in xenograft tumor growth when motesanib was combined with docetaxel (MDA-MB-231 tumors) or with the estrogen receptor modulator tamoxifen (MCF-7 tumors), compared with either treatment alone, but not when combined with doxorubicin (Cal-51 tumors). Reference: Clin Cancer Res. 2009 Jan 1;15(1):110-8. https://pubmed.ncbi.nlm.nih.gov/19118038/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 1.0 | 1.76 | |
| DMSO | 56.5 | 99.22 | |
| DMSO:PBS (pH 7.2) (1:9) | 0.1 | 0.18 | |
| Water | 5.0 | 8.78 |
The following data is based on the product molecular weight 569.4475 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Kaya TT, Altun A, Turgut NH, Ataseven H, Koyluoglu G. Effects of a Multikinase Inhibitor Motesanib (AMG 706) Alone and Combined with the Selective DuP-697 COX-2 Inhibitor on Colorectal Cancer Cells. Asian Pac J Cancer Prev. 2016;17(3):1103-10. doi: 10.7314/apjcp.2016.17.3.1103. PMID: 27039732. 2. 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. doi: 10.1158/0008-5472.CAN-05-4665. PMID: 16951187. 3. 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. doi: 10.1158/1078-0432.CCR-09-3385. Epub 2010 May 27. PMID: 20507929; PMCID: PMC3216115. 4. 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. doi: 10.1158/1078-0432.CCR-08-1155. PMID: 19118038. |
| In vitro protocol: | 1. Kaya TT, Altun A, Turgut NH, Ataseven H, Koyluoglu G. Effects of a Multikinase Inhibitor Motesanib (AMG 706) Alone and Combined with the Selective DuP-697 COX-2 Inhibitor on Colorectal Cancer Cells. Asian Pac J Cancer Prev. 2016;17(3):1103-10. doi: 10.7314/apjcp.2016.17.3.1103. PMID: 27039732. 2. 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. doi: 10.1158/0008-5472.CAN-05-4665. PMID: 16951187. |
| In vivo protocol: | 1. 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. doi: 10.1158/1078-0432.CCR-09-3385. Epub 2010 May 27. PMID: 20507929; PMCID: PMC3216115. 2. 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. doi: 10.1158/1078-0432.CCR-08-1155. PMID: 19118038. |
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