Motesanib phosphate
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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.


Chemical Structure

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Motesanib phosphate
CAS# 857876-30-3 (phosphate)

Theoretical Analysis

MedKoo Cat#: 123214
Name: Motesanib phosphate
CAS#: 857876-30-3 (phosphate)
Chemical Formula: C22H27N5O8P2
Exact Mass:
Molecular Weight: 551.4325
Elemental Analysis: C, 47.92; H, 4.94; N, 12.70; O, 23.21; P, 11.23

Price and Availability

Size Price Availability Quantity
25.0mg USD 150.0 2 Weeks
50.0mg USD 250.0 2 Weeks
100.0mg USD 450.0 2 Weeks
200.0mg USD 750.0 2 Weeks
500.0mg USD 1450.0 2 Weeks
1.0g USD 2150.0 2 Weeks
2.0g USD 3650.0 2 Weeks
5.0g USD 5850.0 2 Weeks
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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

Preparing Stock Solutions

The following data is based on the product molecular weight 551.4325 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.

Recalculate based on batch purity %
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

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1: Kubota K, Yoshioka H, Oshita F, Hida T, Yoh K, Hayashi H, Kato T, Kaneda H, Yamada K, Tanaka H, Ichinose Y, Park K, Cho EK, Lee KH, Lin CB, Yang JC, Hara K, Asato T, Nakagawa K. Phase III, Randomized, Placebo-Controlled, Double-Blind Trial of Motesanib (AMG-706) in Combination With Paclitaxel and Carboplatin in East Asian Patients With Advanced Nonsquamous Non-Small-Cell Lung Cancer. J Clin Oncol. 2017 Nov 10;35(32):3662-3670. doi: 10.1200/JCO.2017.72.7297. Epub 2017 Sep 13. PubMed PMID: 28902534.

2: Torok S, Rezeli M, Kelemen O, Vegvari A, Watanabe K, Sugihara Y, Tisza A, Marton T, Kovacs I, Tovari J, Laszlo V, Helbich TH, Hegedus B, Klikovits T, Hoda MA, Klepetko W, Paku S, Marko-Varga G, Dome B. Limited Tumor Tissue Drug Penetration Contributes to Primary Resistance against Angiogenesis Inhibitors. Theranostics. 2017 Jan 1;7(2):400-412. doi: 10.7150/thno.16767. eCollection 2017. PubMed PMID: 28042343; PubMed Central PMCID: PMC5197073.

3: Skouras VS, Maragkos C, Grapsa D, Syrigos KN. Targeting Neovasculature with Multitargeted Antiangiogenesis Tyrosine Kinase Inhibitors in Non-small Cell Lung Cancer. BioDrugs. 2016 Oct;30(5):421-439. Review. PubMed PMID: 27670779.

4: Song J, Kim SB, Kim KH, Kim TN, Lee KH. A case report of motesanib-induced biliary sludge formation causing obstructive cholangitis with acute pancreatitis treated by endoscopic sphincterotomy. Medicine (Baltimore). 2016 Sep;95(37):e4645. doi: 10.1097/MD.0000000000004645. PubMed PMID: 27631212; PubMed Central PMCID: PMC5402555.

5: Yamauchi F, Kamioka Y, Yano T, Matsuda M. In Vivo FRET Imaging of Tumor Endothelial Cells Highlights a Role of Low PKA Activity in Vascular Hyperpermeability. Cancer Res. 2016 Sep 15;76(18):5266-76. doi: 10.1158/0008-5472.CAN-15-3534. Epub 2016 Aug 3. PubMed PMID: 27488524.

6: Gosselin NH, Mouksassi MS, Lu JF, Hsu CP. Population pharmacokinetic modeling of motesanib and its active metabolite, M4, in cancer patients. Clin Pharmacol Drug Dev. 2015 Nov;4(6):463-72. doi: 10.1002/cpdd.196. Epub 2015 Jul 23. PubMed PMID: 27137719.

7: 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. PubMed PMID: 27039732.

8: Tarshis S, Maltzahn J, Loomis Z, Irwin DC. Preventing High Altitude Cerebral Edema in Rats with Repurposed Anti-Angiogenesis Pharmacotherapy. Aerosp Med Hum Perform. 2016 Dec 1;87(12):1031-1035. doi: 10.3357/AMHP.4571.2016. PubMed PMID: 28323589.

9: Dunna NR, Kandula V, Girdhar A, Pudutha A, Hussain T, Bandaru S, Nayarisseri A. High Affinity Pharmacological Profiling of Dual Inhibitors Targeting RET and VEGFR2 in Inhibition of Kinase and Angiogeneis Events in Medullary Thyroid Carcinoma. Asian Pac J Cancer Prev. 2015;16(16):7089-95. PubMed PMID: 26514495.

10: Gao C, Grøtli M, Eriksson LA. Characterization of interactions and pharmacophore development for DFG-out inhibitors to RET tyrosine kinase. J Mol Model. 2015 Jul;21(7):167. doi: 10.1007/s00894-015-2708-z. Epub 2015 Jun 6. PubMed PMID: 26044359.

11: Caglevic C, Grassi M, Raez L, Listi A, Giallombardo M, Bustamante E, Gil-Bazo I, Rolfo C. Nintedanib in non-small cell lung cancer: from preclinical to approval. Ther Adv Respir Dis. 2015 Aug;9(4):164-72. doi: 10.1177/1753465815579608. Epub 2015 Apr 7. Review. PubMed PMID: 25855060.

12: PLOS ONE Staff. Correction: challenges in developing a validated biomarker for angiogenesis inhibitors: the motesanib experience. PLoS One. 2015 Mar 26;10(3):e0121162. doi: 10.1371/journal.pone.0121162. eCollection 2015. PubMed PMID: 25811784; PubMed Central PMCID: PMC4374716.

13: Tebbutt N, Kotasek D, Burris HA, Schwartzberg LS, Hurwitz H, Stephenson J, Warner DJ, Chen L, Hsu CP, Goldstein D. Motesanib with or without panitumumab plus FOLFIRI or FOLFOX for the treatment of metastatic colorectal cancer. Cancer Chemother Pharmacol. 2015 May;75(5):993-1004. doi: 10.1007/s00280-015-2694-y. Epub 2015 Mar 15. PubMed PMID: 25772756.

14: Greenall SA, Donoghue JF, Van Sinderen M, Dubljevic V, Budiman S, Devlin M, Street I, Adams TE, Johns TG. EGFRvIII-mediated transactivation of receptor tyrosine kinases in glioma: mechanism and therapeutic implications. Oncogene. 2015 Oct 8;34(41):5277-87. doi: 10.1038/onc.2014.448. Epub 2015 Feb 9. PubMed PMID: 25659577.

15: Gruber JJ, Colevas AD. Differentiated thyroid cancer: focus on emerging treatments for radioactive iodine-refractory patients. Oncologist. 2015 Feb;20(2):113-26. doi: 10.1634/theoncologist.2014-0313. Epub 2015 Jan 23. Review. PubMed PMID: 25616432; PubMed Central PMCID: PMC4319630.

16: Lkhoyaali S, Benhmida S, Ait Elhaj M, Layachi M, Bensouda Y, Errihani H. [Targeted therapy in thyroid cancer: Towards a treatment card]. Pathol Biol (Paris). 2015 Feb;63(1):1-6. doi: 10.1016/j.patbio.2014.11.003. Epub 2014 Dec 30. Review. French. PubMed PMID: 25555494.

17: Hong DS, Kurzrock R, Mulay M, Rasmussen E, Wu BM, Bass MB, Zhong ZD, Friberg G, Rosen LS. A phase 1b, open-label study of trebananib plus bevacizumab or motesanib in patients with solid tumours. Oncotarget. 2014 Nov 30;5(22):11154-67. PubMed PMID: 25525888; PubMed Central PMCID: PMC4294348.

18: Bass MB, Yao B, Hei YJ, Ye Y, Davis GJ, Davis MT, Kaesdorf BA, Chan SS, Patterson SD. Challenges in developing a validated biomarker for angiogenesis inhibitors: the motesanib experience. PLoS One. 2014 Oct 14;9(10):e108048. doi: 10.1371/journal.pone.0108048. eCollection 2014. Erratum in: PLoS One. 2015;10(3):e0121162. PubMed PMID: 25314641; PubMed Central PMCID: PMC4196848.

19: Kim JG. Molecular pathogenesis and targeted therapies in well-differentiated thyroid carcinoma. Endocrinol Metab (Seoul). 2014 Sep;29(3):211-6. doi: 10.3803/EnM.2014.29.3.211. Review. PubMed PMID: 25309777; PubMed Central PMCID: PMC4192816.

20: Wang YJ, Zhang YK, Kathawala RJ, Chen ZS. Repositioning of Tyrosine Kinase Inhibitors as Antagonists of ATP-Binding Cassette Transporters in Anticancer Drug Resistance. Cancers (Basel). 2014 Sep 29;6(4):1925-52. doi: 10.3390/cancers6041925. Review. PubMed PMID: 25268163; PubMed Central PMCID: PMC4276951.