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L-5814 Linsitinib, Free Base, >99%       Prices Reduced (April 2013)      NEW!

Synonyms:  [OSI-906] [OSI 906AA] [OSI 906] [OSI906] [OSI-906AA] [OSI906AA]

M.W. 421.49

C26H23N5O

[867160-71-2]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 50 mg/mL; soluble in ethanol at 3 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 2-5 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.   Disposal:  A

Find and View a Certificate of Analysis for this product

View the MSDS for this product

• Linsitinib, also known as OSI-906, is a novel, potent small-molecule dual insulin-like growth factor-1 receptor (IGF-1R)/insulin receptor (IR) kinase inhibitor.

• Linsitinib inhibited IGF-1R and IR kinases with IC50 values of 35 nM and 75 nM, respectively.  Linsitinib potently and selectively blocked autophosphorylation of both human IGF-1R and IR, inhibited the proliferation of a variety of tumor cell lines in vitro, and displayed robust in vivo anti-tumor efficacy in an IGF-1R-driven xenograft model when administered orally.  Mulvihill, M.J., et al.  "Discovery of OSI-906:  a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor."  Future Med. Chem. 1:  1153-1171 (2009).

• Linsitinib showed superior efficacy compared with MAB391, a selective anti-IGF-1R antibody, in human tumor xenograft models in which both IGF-1R and IR were phosphorylated.  Buck, E., et al.  "Compensatory insulin receptor (IR) activation on inhibition of insulin-like growth factor-1 receptor (IGF-1R):  rationale for cotargeting IGF-1R and IR in cancer."  Mol. Cancer Ther. 9:  2652-2664 (2010).

• Following a single dose of linsitinib, 18FDG-PET was shown to serve as a rapid, noninvasive pharmacodynamic biomarker of IGF-1R/IR inhibition.  McKinley, E.T., et al.  "18FDG-PET predicts pharmacodynamic response to OSI-906, a dual IGF-1R/IR inhibitor, in preclinical mouse models of lung cancer."  Clin. Cancer Res. 17:  3332-3340 (2011).

• IGF-1 was shown to be overexpressed in low-grade serous ovarian carcinoma (SOC) when compared with serous borderline ovarian tumors (SBOTs) and high-grade SOCs.  Low-grade SOC cell lines were more sensitive to IGF-1 stimulation and IGF-1R inhibition than were high-grade lines.  Therefore, the IGF-1 pathway is a potential therapeutic target in low-grade SOC.  King, E.R., et al.  "The insulin-like growth factor 1 pathway is a potential therapeutic target for low-grade serous ovarian carcinoma."  Gynecol. Oncol. 123:  13-18 (2011).

• Linsitinib blocked IGF-1 signaling in LCC6 xenograft tumors in vivo.  When given once a week, combined administration simultaneously of OSI-906 and doxorubicin significantly improved the anti-tumor effect of doxorubicin.  Zeng X., et al.  "Enhancement of doxorubicin cytotoxicity of human cancer cells by tyrosine kinase inhibition of insulin receptor and type I IGF receptor."  Breast Cancer Res. Treat. 133:  117-126 (2012).

• Therapeutic targeting of both IR and IGF-1R by linsitinib was shown to be more effective than targeting IGF-1R alone by MAB391 in abrogating resistance to endocrine therapy in breast cancer.  Fox, E.M., et al.  "A kinome-wide screen identifies the insulin/IGF-1 receptor pathway as a mechanism of escape from hormone dependence in breast cancer."  Cancer Res. 71:  6773-6784 (2011).

• Epithelial-mesenchymal transition (EMT) was demonstrated to predict hepatocellular carcinoma cell sensitivity to linsitinib, as the epithelial phenotype was strongly associated with expression of IGF-2 and IR, and activation of IGF-1R and IR.  Induction of EMT by TGFβ reduced sensitivity to linsitinib.  Zhao, H., et al.  "Epithelial-mesenchymal transition predicts sensitivity to the dual IGF-1R/IR inhibitor OSI-906 in hepatocellular carcinoma cell lines."  Mol. Cancer Ther. 11:  503-513 (2012)

• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.

** Our prices are lower than other vendors', but there is no compromise in quality.  Read how we are able to accomplish this:  Product Quality Discussion.

NOTES:
1.  The purpose of our competitor price comparison tables is to enable our visitors to compare the prices and purities of products of nominally equivalent quality, for vendors whose price and purity claims are openly available from a website or catalog (without a need for the customer to contact the vendor and request a quotation in order to obtain a price and purity for a standard product size).  However, the quality comparisons in these tables are not absolute:  although our product purities are uniformly very high and are established by careful testing of every lot in our laboratories, we cannot and do not vouch for the purities claimed by other vendors in these competitor price comparison tables.  (We do carry out occasional testing of other vendors' products -- see below --  and we have found many instances where vendors' product purities are far below their claimed levels.)  Effective April 1, 2011, our price comparison tables only include products where a purity commitment is found together with sizes and prices on at least one page of the vendor's web site.

2.  Researching and compiling sizes and prices for the >160 competitive vendors and more than 175 products is an expensive and tedious task for our small company.  Thus, we typically only perform revisions of these tables annually or less frequently.  The date and source of each competitive vendor's prices is indicated at the bottom of this page.  Obviously, we make no guarantee that competitive vendor prices will remain unchanged in the interval between our annual revisions.  We may occasionally update individual competitive vendor information and add new competitive vendors as we locate them.

3.  In some circumstances we permanently remove vendors from our price comparison tables.  Circumstances that lead to permanent removal are: 

A.  If a vendor does not honor its advertised price (ignoring small price increases) for one or more products when an order is attempted.  Example:  a vendor listed a compound at $808 for 10 grams on its website price list, but quoted $4,500 per 10 grams upon our inquiry.  That vendor has been permanently removed from our price comparison tables.

B.  If, on a product-by-product basis, our analyses of a vendor's product show purities more than a few percent below the vendor's advertised purities.  Example:  a vendor advertises a purity for 97% for a compound, but repeated elemental analyses show a minimum of 9% inorganic material present, beyond any salt counterion.  Another example: an HPLC analysis at a relevant UV detector wavelength shows 92% purity for a vendor's product for which 98% purity is claimed.  We realize of course that UV absorbances for impurities can be higher than for the main compound, but our products meet our purity commitment of typically >99% irrespective of absorbance factors for impurities, and we apply that standard to products from other vendors.

C.  Again on a product-by-product basis, if a vendor makes no purity claim for a given product, then their product is not shown on that product table.

D.  If we find that, as a pattern, several of a competitive vendor's products fail to meet their advertised purity commitments by significant margins or if a vendor does not provide standard and consistent purity claims for several of its products, then that vendor is permanently removed from all of our competitor price tables.

E.  Finally, if we determine that a vendor has provided fraudulent information on its website, in its literature or on a certificate of analysis, that vendor is permanently removed from all of our price comparison tables.

4.  IMPORTANT:  The presence of a competitive vendor entry in our price comparison tables does not necessarily mean that we have analyzed any of that vendor's products for purity; indeed, in most cases we have not.

5.  Please note:  where necessary, competitor prices are rounded to the nearest whole dollar.

To the best of our knowledge, the prices listed above for our competitors' products were correct as of the dates listed below for the sources of our annual price information update process.

Pricing Sources and Dates:  LC Labs - Current, Active Biochem - website - Mar 2013, BioVision - website - May 2013, PharmBlock - website - Apr 2013, ChemieTek - website - Jun 2013, Axon Medchem - website - Mar 2013, JiHe Pharmaceutica - website - Jan 2013, VDM Biochemicals - website - Dec 2012, biorbyt.com - website - Sep 2012, Taizhou Crene Biotechnology - website - Jan 2013, HuoLi Biochem - website - Jan 2013, Acesobio - website - Jan 2013, Cellagen Technology - website - May 2013, Reliable ChemTech - Google Sites - Jan 2013, AbMole BioScience - website - May 2013, MedKoo BioSciences - website - Apr 2013, Medchem Express - website - Jun 2013, AdooQ BioScience - website - Jan 2013, ChemScene - website - Jan 2013, Phoenix Pharmaceuticals - website - Jan 2013, Kinasechem - website - Apr 2013.