GDC-0941, Free Base **

产品名称：GDC-0941, Free Base
产品货号：LC  G-9252
产品规格：1 G
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.
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

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