EOS Med Chem produce Motesanib CAS:453562-69-1, assay 99.2% to be China biggest, NMR, MS, COA is OK.
2017 China CPHI: E1M35
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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. (NCI Thesaurus).
Name: Motesanib
CAS#: 453562-69-1 (Motesanib); 857876-30-3 (Motesanib diphosphate) Chemical Formula: C22H23N5O Exact Mass: 373.1902 Molecular Weight: 373.46 Elemental Analysis: C, 70.76; H, 6.21; N, 18.75; O, 4.28
Synonym: AMG 706; AMG706; AMG706; motesanib
IUPAC/Chemical Name: N-(3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-2-[(pyridin-4- ylmethyl)amino]pyridine-3-carboxamide
InChi Key: RAHBGWKEPAQNFF-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H23N5O/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/h3-12,26H,13-14H2,1-2H3,(H,24,25)(H,27,28)
SMILES Code: O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC4=C(C=C3)C(C)(C)CN4
Appearance: White to off-white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Certificate of Analysis: View CoA
QC Data: View QC data
Safety Data Sheet (MSDS): View Material Safety Data Sheet (MSDS)
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, not in water
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).
Harmonized System Code: 293490
REFERENCES
1: Kruser TJ, Wheeler DL, Armstrong EA, Iida M, Kozak KR, van der Kogel AJ, Bussink J, Coxon A, Polverino A, Harari P. Augmentation of Radiation Response by Motesanib, A Multikinase Inhibitor That Targets Vascular Endothelial Growth Factor Receptors. Clin Cancer Res. 2010 May 27. [Epub ahead of print] PubMed PMID: 20507929.
2: Rosen PJ, Sweeney CJ, Park DJ, Beaupre DM, Deng H, Leitch IM, Shubhakar P, Zhu M, Oliner KS, Anderson A, Yee LK. A phase Ib study of AMG 102 in combination with bevacizumab or motesanib in patients with advanced solid tumors. Clin Cancer Res. 2010 May 1;16(9):2677-87. Epub 2010 Apr 20. PubMed PMID: 20406832.
3: Fujisaka Y, Yamada Y, Yamamoto N, Shimizu T, Fujiwara Y, Yamada K, Tamura T, Watanabe H, Sun YN, Bass MB, Seki M. Phase 1 study of the investigational, oral angiogenesis inhibitor motesanib in Japanese patients with advanced solid tumors. Cancer Chemother Pharmacol. 2010 Jan 28. [Epub ahead of print] PubMed PMID: 20107802.
4: Keefe SM, Cohen MA, Brose MS. Targeting vascular endothelial growth factor receptor in thyroid cancer: the intracellular and extracellular implications. Clin Cancer Res. 2010 Feb 1;16(3):778-83. Epub 2010 Jan 26. Review. PubMed PMID: 20103668.
5: Blumenschein GR Jr, Reckamp K, Stephenson GJ, O'Rourke T, Gladish G, McGreivy J, Sun YN, Ye Y, Parson M, Sandler A. Phase 1b study of motesanib, an oral angiogenesis inhibitor, in combination with carboplatin/paclitaxel and/or panitumumab for the treatment of advanced non-small cell lung cancer. Clin Cancer Res. 2010 Jan 1;16(1):279-90. Epub 2009 Dec 22. PubMed PMID: 20028752.
6: Sherman SI. Tyrosine kinase inhibitors and the thyroid. Best Pract Res Clin Endocrinol Metab. 2009 Dec;23(6):713-22. Review. PubMed PMID: 19942148.
7: Sawaki A, Yamada Y, Komatsu Y, Kanda T, Doi T, Koseki M, Baba H, Sun YN, Murakami K, Nishida T. Phase II study of motesanib in Japanese patients with advanced gastrointestinal stromal tumors with prior exposure to imatinib mesylate. Cancer Chemother Pharmacol. 2010 Apr;65(5):961-7. Epub 2009 Aug 19. PubMed PMID: 19690858; PubMed Central PMCID: PMC2824121.
8: Sugawara M, Geffner DL, Martinez D, Hershman JM. Novel treatment of medullary thyroid cancer. Curr Opin Endocrinol Diabetes Obes. 2009 Oct;16(5):367-72. Review. PubMed PMID: 19633548.
9: Schlumberger MJ, Elisei R, Bastholt L, Wirth LJ, Martins RG, Locati LD, Jarzab B, Pacini F, Daumerie C, Droz JP, Eschenberg MJ, Sun YN, Juan T, Stepan DE, Sherman SI. Phase II study of safety and efficacy of motesanib in patients with progressive or symptomatic, advanced or metastatic medullary thyroid cancer. J Clin Oncol. 2009 Aug 10;27(23):3794-801. Epub 2009 Jun 29. PubMed PMID: 19564535.
10: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Mar;31(2):107-46. PubMed PMID: 19455266.
11: Li C, Kuchimanchi M, Hickman D, Poppe L, Hayashi M, Zhou Y, Subramanian R, Kumar G, Surapaneni S. In vitro metabolism of the novel, highly selective oral angiogenesis inhibitor motesanib diphosphate in preclinical species and in humans. Drug Metab Dispos. 2009 Jul;37(7):1378-94. Epub 2009 Apr 16. PubMed PMID: 19372226.
12: Malouf G, Baudin E, Soria JC, Schlumberger M. [Advances in the treatment of thyroid cancer in the era of molecularly targeted therapies]. Bull Cancer. 2009 Jan;96(1):95-101. Review. French. PubMed PMID: 19211364.
13: Kiselyov AS, Semenova M, Semenov VV. 3,4-Disubstituted isothiazoles: novel potent inhibitors of VEGF receptors 1 and 2. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1195-8. Epub 2008 Dec 24. PubMed PMID: 19124243.
14: 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. PubMed PMID: 19118038.
15: Diaz-Cano SJ. Motesanib diphosphate in progressive differentiated thyroid cancer. N Engl J Med. 2008 Dec 18;359(25):2727; author reply 2727. PubMed PMID: 19092161.
16: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Oct;30(8):643-72. PubMed PMID: 19088949.
17: Lanzi C, Cassinelli G, Nicolini V, Zunino F. Targeting RET for thyroid cancer therapy. Biochem Pharmacol. 2009 Feb 1;77(3):297-309. Epub 2008 Nov 6. PubMed PMID: 19028457.
18: Azad A, Herbertson RA, Pook D, White S, Mitchell PL, Tebbutt NC. Motesanib diphosphate (AMG 706), an oral angiogenesis inhibitor, demonstrates clinical efficacy in advanced thymoma. Acta Oncol. 2009;48(4):619-21. PubMed PMID: 18979266.
1: Kruser TJ, Wheeler DL, Armstrong EA, Iida M, Kozak KR, van der Kogel AJ, Bussink J, Coxon A, Polverino A, Harari P. Augmentation of Radiation Response by Motesanib, A Multikinase Inhibitor That Targets Vascular Endothelial Growth Factor Receptors. Clin Cancer Res. 2010 May 27. [Epub ahead of print] PubMed PMID: 20507929.
2: Rosen PJ, Sweeney CJ, Park DJ, Beaupre DM, Deng H, Leitch IM, Shubhakar P, Zhu M, Oliner KS, Anderson A, Yee LK. A phase Ib study of AMG 102 in combination with bevacizumab or motesanib in patients with advanced solid tumors. Clin Cancer Res. 2010 May 1;16(9):2677-87. Epub 2010 Apr 20. PubMed PMID: 20406832.
3: Fujisaka Y, Yamada Y, Yamamoto N, Shimizu T, Fujiwara Y, Yamada K, Tamura T, Watanabe H, Sun YN, Bass MB, Seki M. Phase 1 study of the investigational, oral angiogenesis inhibitor motesanib in Japanese patients with advanced solid tumors. Cancer Chemother Pharmacol. 2010 Jan 28. [Epub ahead of print] PubMed PMID: 20107802.
4: Keefe SM, Cohen MA, Brose MS. Targeting vascular endothelial growth factor receptor in thyroid cancer: the intracellular and extracellular implications. Clin Cancer Res. 2010 Feb 1;16(3):778-83. Epub 2010 Jan 26. Review. PubMed PMID: 20103668.
5: Blumenschein GR Jr, Reckamp K, Stephenson GJ, O'Rourke T, Gladish G, McGreivy J, Sun YN, Ye Y, Parson M, Sandler A. Phase 1b study of motesanib, an oral angiogenesis inhibitor, in combination with carboplatin/paclitaxel and/or panitumumab for the treatment of advanced non-small cell lung cancer. Clin Cancer Res. 2010 Jan 1;16(1):279-90. Epub 2009 Dec 22. PubMed PMID: 20028752.
6: Sherman SI. Tyrosine kinase inhibitors and the thyroid. Best Pract Res Clin Endocrinol Metab. 2009 Dec;23(6):713-22. Review. PubMed PMID: 19942148.
7: Sawaki A, Yamada Y, Komatsu Y, Kanda T, Doi T, Koseki M, Baba H, Sun YN, Murakami K, Nishida T. Phase II study of motesanib in Japanese patients with advanced gastrointestinal stromal tumors with prior exposure to imatinib mesylate. Cancer Chemother Pharmacol. 2010 Apr;65(5):961-7. Epub 2009 Aug 19. PubMed PMID: 19690858; PubMed Central PMCID: PMC2824121.
8: Sugawara M, Geffner DL, Martinez D, Hershman JM. Novel treatment of medullary thyroid cancer. Curr Opin Endocrinol Diabetes Obes. 2009 Oct;16(5):367-72. Review. PubMed PMID: 19633548.
9: Schlumberger MJ, Elisei R, Bastholt L, Wirth LJ, Martins RG, Locati LD, Jarzab B, Pacini F, Daumerie C, Droz JP, Eschenberg MJ, Sun YN, Juan T, Stepan DE, Sherman SI. Phase II study of safety and efficacy of motesanib in patients with progressive or symptomatic, advanced or metastatic medullary thyroid cancer. J Clin Oncol. 2009 Aug 10;27(23):3794-801. Epub 2009 Jun 29. PubMed PMID: 19564535.
10: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Mar;31(2):107-46. PubMed PMID: 19455266.
11: Li C, Kuchimanchi M, Hickman D, Poppe L, Hayashi M, Zhou Y, Subramanian R, Kumar G, Surapaneni S. In vitro metabolism of the novel, highly selective oral angiogenesis inhibitor motesanib diphosphate in preclinical species and in humans. Drug Metab Dispos. 2009 Jul;37(7):1378-94. Epub 2009 Apr 16. PubMed PMID: 19372226.
12: Malouf G, Baudin E, Soria JC, Schlumberger M. [Advances in the treatment of thyroid cancer in the era of molecularly targeted therapies]. Bull Cancer. 2009 Jan;96(1):95-101. Review. French. PubMed PMID: 19211364.
13: Kiselyov AS, Semenova M, Semenov VV. 3,4-Disubstituted isothiazoles: novel potent inhibitors of VEGF receptors 1 and 2. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1195-8. Epub 2008 Dec 24. PubMed PMID: 19124243.
14: 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. PubMed PMID: 19118038.
15: Diaz-Cano SJ. Motesanib diphosphate in progressive differentiated thyroid cancer. N Engl J Med. 2008 Dec 18;359(25):2727; author reply 2727. PubMed PMID: 19092161.
16: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Oct;30(8):643-72. PubMed PMID: 19088949.
17: Lanzi C, Cassinelli G, Nicolini V, Zunino F. Targeting RET for thyroid cancer therapy. Biochem Pharmacol. 2009 Feb 1;77(3):297-309. Epub 2008 Nov 6. PubMed PMID: 19028457.
18: Azad A, Herbertson RA, Pook D, White S, Mitchell PL, Tebbutt NC. Motesanib diphosphate (AMG 706), an oral angiogenesis inhibitor, demonstrates clinical efficacy in advanced thymoma. Acta Oncol. 2009;48(4):619-21. PubMed PMID: 18979266.
