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LC Labs/R-3692 Rociletinib, Free Base, >99%/R-3692/25 mg
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发布时间：2025-01-15
- Rociletinib, also known as CO-1686, is an irreversible tyrosine kinase inhibitor with a Ki of 21.5 nM for the EGFR L858R/T790M mutant and a Ki of 303.3 nM for wt EGFR. It inhibited the growth of non-small cell lung cancer (NSCLC) cells expressing mutant EGFR, and it induced apoptosis. It also demonstrated in vivo anti-tumor activity in mice bearing NSCLC tumors with activating EGFR mutations. Walter A.O., et al. \"Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.\" Cancer Discov. 3: 1404-1415 (2013).
- The T790M mutation is the most common reason for acquired resistance to existing EGFR inhibitors in NSCLC. Rociletinib potently inhibited mutant EGFR L858R/T790M with an IC50 < 0.51nM. Rociletinib blocked the growth of T790M-positive NSCLC cells in vitro and in vivo. Walter A.O., et al. \"CO-1686, a novel mutant-selective EGFR inhibitor, overcomes T790M mediated resistance in non-small cell lung cancer (NSCLC).\" http://www.clovisoncology.com/assets/pdf/CO-1686/Clovis-Avila_AACR_2012_CO-1686_Poster_ClovisFINAL_27MAR12.pdf
- A phase I clinical trial in patients with EGFR mutated NSCLC demonstrated that rociletinib was well tolerated, and activity was observed in dose escalation cohorts. Sequist L.V., et al. \"First-in-human evaluation of CO-1686, an irreversible, selective, and potent tyrosine kinase inhibitor of EGFR T790M.\" http://www.clovisoncology.com/files/CLVS_ASCO_2013_poster_CO1686_P1monotx_abstract2524.pdf
- 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.
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发布于 ： 2025-01-15
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