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Exelixis.Inc is a great drug discovery company and invented a list of inhibitors including 880, 147, 765, 518, 652/ 014, 139, 281, 475, 550 and Cabozantinib ( 184). Some inhibitors have already been used in our experiments and some inhibitors is still unknown. It’s still difficult for us to know the information of some inhibitors,including formula and IC50 value. Some researchers dig out the related information and post them on the blog, such as Kinasepro, a great blog. Some great reagent supplier also provide the information.Today, I would give a general review of some of those inhibitors and some information is really difficult to collect. I would also list the information resources so that readers can refer to them and maybe you can find more information. Other inhibitors which I did not mentioned in this poster would appear in the next poster. (1) 880 518,a MET inhibitor In the website of Exelixis.Inc, they describe the inhibitor as a potent inhibitor of MET and VEGFR2 which play cooperative roles in promoting tumor growth and angiogenesis. Actually, according to the article published in 2009 from cancer research, researchers reported a list of targets of 880. For the RTKs, 880 can inhibit MET and Ron, which are both HGF receptor family kinases, with IC50 of 0.4 nM and 3 nM. Other RTKs, such as KDR, Flt-1, and Flt-4, can be inhibited by 880 with IC50 values of 0.9, 6.8, and 2.8 nmol/L. [1] (2) 147 147, a PI3K inhibitor 147 is a selective PI3K inhibitor. It just inhibit class I PI3K isoform. According to the article “Targeting Aberrant PI3K Pathway Signaling With 147, a Potent, Selective, and Orally Bioavailable PI3K Inhibitor”, researchers report the IC50 value of 147. 147 can inhibit PI3K-alpha, PI3K-beta, PI3K-delta and PI3K-gamma with IC50 of 39, 383, 36 and 23 nM. Now, according to the information from the website of Exelixis.Inc, the inhibitor have already entered phase II. Phase Clinical Trials Status Phase 2 Study of 147 in Advanced or Recurrent Endometrial Cancer Recruiting Phase 1b/2 Study of 147 in Combination With Trastuzumab or Paclitaxel and Trastuzumab in Subjects With Metastatic Breast Cancer Who Have Progressed on a Previous Trastuzumab-based Regimen Recruiting Phase 1b/2 Safety Study of 147 in Combination With Erlotinib in Adults With Solid Tumors Recruiting Phase 1b/2 Safety Study of 147 in Combination With Paclitaxel and Carboplatin in Adults With Solid Tumors Recruiting Phase 1 Study of the Safety and Pharmacokinetics of 147 in Adults With Solid Tumors or Lymphoma Recruiting (3) 765 765,a PI3K/mTOR dual inhibitor 765 is a PI3K/mTOR dual inhibitor and 765 can inhibit PI3K-alpha, PI3K-beta, PI3K-gamma and PI3K-delta with IC50 of 39, 113, 9 and 43 nM. And 765 also inhibit mTOR with IC50 of 157 nM. Now the inhibitor is in the phase I. Phase Clinical Trials Status Phase 1b/2 A Study of 765 in Combination With Temozolomide in Adults With Malignant Gliomas Recruiting Phase 1b/2 Safety Study of 765 in Combination With Erlotinib in Adults With Solid Tumors Recruiting Phase 1 Study of the Safety and Pharmacokinetics of 765 in Adults With Solid Tumors Recruiting (4) 518 The structure of 518 is difficult to get. I have check the articles published in recent years and I got no information. But the great blog, Kinasespro, have posted some information about 518. And I got the structure from the Kinasepro. 518, a MEK inhibitor 518, a MEK inhibitor But I remembered that I have already drew the structure. And I found out the structure is the same with GDC-0973. GDC-0973,a MEK inhibitor You can compare them and they are the same. GC-0973 ( 518) is a potent MEK inhibitor with IC50 of 4.2 nM.[2] In the next poster, I would continues to talking about this topic and introducing more inhibitors from Exelixis.Inc. We has established long-term and stable relationships with more than 10,000 customers from pharmaceutical and biotech companies, universities and research institutions. We have high quality inhibitors like Sunitinib, Temsirolimus, Compound Libraries & more. We have headquarters in both United States and Europe, and also has 38 distributors worldwide. We provide overnight delivery in North America and Europe.
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