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G-9252 GDC-0941, Free Base, >99%       Prices Reduced (December 2011)

[New Generic Name:  Pictilisib]

[GDC 0941] [GDC0941]

M.W. 513.64

C23H27N7O3S2

[957054-30-7]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 66 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-50 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

• GDC-0941 is a phosphatidylinositol 3-kinase (PI3K) inhibitor.  Folkes, A.J., et al.  "The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer."  J. Med. Chem. 51:  5522-5532 (2008).

• GDC-0941 inhibited the growth of >70% of breast cancer cell lines tested, with EC50's <1 µM.  GDC-0941 also demonstrated antitumor activity in preclinical models of breast cancer.  Yao, E., et al.  "Suppression of HER2/HER3-mediated growth of breast cancer cells with combinations of GDC-0941 PI3K inhibitor, trastuzumab, and pertuzumab."  Clin. Cancer Res. 15:  4147-4156 (2009).

• The combination of GDC-0941 with trastuzumab is highly efficacious in the treatment of cancer cells in vitro and tumors in vivo.  GDC-0941 also has antitumor activity in the treatment of trastuzumab-resistant cells and tumors.  Junttila, T.T., et al.  "Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941."  Cancer Cell 15:  429-440 (2009).

• GDC-0941 inhibits the activity of recombinant PI3K in vitro with IC50's of 0.003 µM (P110α), 0.033 µM (P110β), 0.003 µM (P110δ), 0.075 µM (P110γ), 0.58 µM (mTOR) and 1.23 µM (DNA-PK).  GDC-0941 inhibited the growth of tumor cells in vitro with IC50's of 0.95 µM (U87MG), 0.07 µM (IGROV-1), 0.15 µM (DETROIT 562), 0.28 µM (PC3) and 0.54 µM (SKOV-3).  GDC-0941 also inhibited the growth of U87 MG glioblastoma xenografts and IGROV-1 ovarian cancer xenografts in mice.  Raynaud, F.I., et al.  "Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941."  Mol. Cancer Ther. 8:  1725-1738 (2009).

• A CAS number previously in use for this compound, 1146702-55-7, has been deleted by Chemical Abstracts Service.

• Sold for laboratory or manufacturing purposes only; not for human, medical, 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 - Apr 2012, BioVision - website - Mar 2012, Cambridge BioScience - website - Mar 2012, ChemieTek - website - Dec 2011, Axon Medchem - website - Mar 2012, Applied StemCell - website - Jan 2012, Stemgent - website - Feb 2012, Chemdea - website - Dec 2011, JiHe Pharmaceutica - website - Dec 2011, ShangHai Biochempartner - website - Dec 2011, antibodies-online - website - Dec 2011, biorbyt.com - website - Mar 2012, Reagents Direct - website - Dec 2011, biokits.com - website - Dec 2011, HuoLi Biochem - website - Dec 2011, Cellagen Technology - website - Dec 2011, Reliable ChemTech - Google Sites - May 2012, BPS Bioscience - website - Dec 2011, AbMole BioScience - website - Mar 2012, SynChem - website - Jan 2012, Medchem Express - website - Apr 2012, AdooQ BioScience - website - Apr 2012, EMMX BioChemicals - website - May 2012.

^† Note:  Active Biochem's product A-1017, Axon Medchem's product Axon 1377, Jihe Pharmaceutica's product JH-1017, ShangHai Biochempartner's product BCP0001, antibodies-online product ABIN412227, and HuoLi Biochem's product A-1017 are the bismesylate salt form of this compound.