Foretinib phosphate

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MedKoo CAT#: 575624

CAS#: 1226999-07-0 (phosphate)

Description: Foretinib phosphate is an orally bioavailable small molecule with potential antineoplastic activity. MET/VEGFR2 inhibitor GSK1363089 binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers.

Chemical Structure

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Foretinib phosphate
CAS# 1226999-07-0 (phosphate)
Instruction

Theoretical Analysis

MedKoo Cat#: 575624
Name: Foretinib phosphate
CAS#: 1226999-07-0 (phosphate)
Chemical Formula: C34H40F2N4O14P2
Exact Mass: 828.20
Molecular Weight: 828.650
Elemental Analysis: C, 49.28; H, 4.87; F, 4.59; N, 6.76; O, 27.03; P, 7.48

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 1226999-07-0 (phosphate)   849217-64-7 (free base)  

Synonym: Foretinib phosphate

IUPAC/Chemical Name: N-(3-fluoro-4-((6-methoxy-7-(3-morpholinopropoxy)quinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide bis(phosphate)

InChi Key: PSMCUKNQAPSTHQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C34H34F2N4O6.2H3O4P/c1-43-30-20-25-27(21-31(30)45-16-2-13-40-14-17-44-18-15-40)37-12-9-28(25)46-29-8-7-24(19-26(29)36)39-33(42)34(10-11-34)32(41)38-23-5-3-22(35)4-6-23;2*1-5(2,3)4/h3-9,12,19-21H,2,10-11,13-18H2,1H3,(H,38,41)(H,39,42);2*(H3,1,2,3,4)

SMILES Code: COc1cc2c(Oc3ccc(NC(=O)C4(CC4)C(=O)Nc5ccc(F)cc5)cc3F)ccnc2cc1OCCCN6CCOCC6.OP(=O)(O)O.OP(=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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 828.65 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Bénard J. [ROS1 fusion proteins, targets of foretinib]. Bull Cancer. 2014 Jan 1;101(1):4. French. PubMed PMID: 24649496.

2: Davare MA, Saborowski A, Eide CA, Tognon C, Smith RL, Elferich J, Agarwal A, Tyner JW, Shinde UP, Lowe SW, Druker BJ. Foretinib is a potent inhibitor of oncogenic ROS1 fusion proteins. Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19519-24. doi: 10.1073/pnas.1319583110. Epub 2013 Nov 11. PubMed PMID: 24218589; PubMed Central PMCID: PMC3845150.

3: Shah MA, Wainberg ZA, Catenacci DV, Hochster HS, Ford J, Kunz P, Lee FC, Kallender H, Cecchi F, Rabe DC, Keer H, Martin AM, Liu Y, Gagnon R, Bonate P, Liu L, Gilmer T, Bottaro DP. Phase II study evaluating 2 dosing schedules of oral foretinib (GSK1363089), cMET/VEGFR2 inhibitor, in patients with metastatic gastric cancer. PLoS One. 2013;8(3):e54014. doi: 10.1371/journal.pone.0054014. Epub 2013 Mar 14. PubMed PMID: 23516391; PubMed Central PMCID: PMC3597709.

4: Logan TF. Foretinib (XL880): c-MET inhibitor with activity in papillary renal cell cancer. Curr Oncol Rep. 2013 Apr;15(2):83-90. doi: 10.1007/s11912-013-0299-3. Review. PubMed PMID: 23408121.

5: Choueiri TK, Vaishampayan U, Rosenberg JE, Logan TF, Harzstark AL, Bukowski RM, Rini BI, Srinivas S, Stein MN, Adams LM, Ottesen LH, Laubscher KH, Sherman L, McDermott DF, Haas NB, Flaherty KT, Ross R, Eisenberg P, Meltzer PS, Merino MJ, Bottaro DP, Linehan WM, Srinivasan R. Phase II and biomarker study of the dual MET/VEGFR2 inhibitor foretinib in patients with papillary renal cell carcinoma. J Clin Oncol. 2013 Jan 10;31(2):181-6. doi: 10.1200/JCO.2012.43.3383. Epub 2012 Dec 3. PubMed PMID: 23213094; PubMed Central PMCID: PMC3532390.

6: Shapiro GI, McCallum S, Adams LM, Sherman L, Weller S, Swann S, Keer H, Miles D, Müller T, Lorusso P. A Phase 1 dose-escalation study of the safety and pharmacokinetics of once-daily oral foretinib, a multi-kinase inhibitor, in patients with solid tumors. Invest New Drugs. 2013 Jun;31(3):742-50. doi: 10.1007/s10637-012-9881-z. Epub 2012 Oct 6. PubMed PMID: 23054208.

7: Seiwert T, Sarantopoulos J, Kallender H, McCallum S, Keer HN, Blumenschein G Jr. Phase II trial of single-agent foretinib (GSK1363089) in patients with recurrent or metastatic squamous cell carcinoma of the head and neck. Invest New Drugs. 2013 Apr;31(2):417-24. doi: 10.1007/s10637-012-9861-3. Epub 2012 Aug 24. PubMed PMID: 22918720; PubMed Central PMCID: PMC3589657.

8: Huynh H, Ong R, Soo KC. Foretinib demonstrates anti-tumor activity and improves overall survival in preclinical models of hepatocellular carcinoma. Angiogenesis. 2012 Mar;15(1):59-70. doi: 10.1007/s10456-011-9243-z. Epub 2011 Dec 21. PubMed PMID: 22187171.

9: Dufies M, Jacquel A, Robert G, Cluzeau T, Puissant A, Fenouille N, Legros L, Raynaud S, Cassuto JP, Luciano F, Auberger P. Mechanism of action of the multikinase inhibitor Foretinib. Cell Cycle. 2011 Dec 1;10(23):4138-48. doi: 10.4161/cc.10.23.18323. Epub 2011 Dec 1. PubMed PMID: 22101270.

10: Kataoka Y, Mukohara T, Tomioka H, Funakoshi Y, Kiyota N, Fujiwara Y, Yashiro M, Hirakawa K, Hirai M, Minami H. Foretinib (GSK1363089), a multi-kinase inhibitor of MET and VEGFRs, inhibits growth of gastric cancer cell lines by blocking inter-receptor tyrosine kinase networks. Invest New Drugs. 2012 Aug;30(4):1352-60. doi: 10.1007/s10637-011-9699-0. Epub 2011 Jun 8. PubMed PMID: 21655918.