79698-53-6Relevant articles and documents
Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R
Czako, Barbara,Marszalek, Joseph. R.,Burke, Jason P.,Mandal, Pijus,Leonard, Paul G.,Cross, Jason B.,Mseeh, Faika,Jiang, Yongying,Chang, Edward Q.,Suzuki, Erika,Kovacs, Jeffrey J.,Feng, Ningping,Gera, Sonal,Harris, Angela L.,Liu, Zhen,Mullinax, Robert A.,Pang, Jihai,Parker, Connor A.,Spencer, Nakia D.,Yu, Simon S.,Wu, Qi,Tremblay, Martin R.,Mikule, Keith,Wilcoxen, Keith,Heffernan, Timothy P.,Draetta, Giulio F.,Jones, Philip
, p. 9888 - 9911 (2020/10/19)
Tumor-associated macrophages (TAMs) have a significant presence in the tumor stroma across multiple human malignancies and are believed to be beneficial to tumor growth. Targeting CSF1R has been proposed as a potential therapy to reduce TAMs, especially the protumor, immune-suppressive M2 TAMs. Additionally, the high expression of CSF1R on tumor cells has been associated with poor survival in certain cancers, suggesting tumor dependency and therefore a potential therapeutic target. The CSF1-CSF1R signaling pathway modulates the production, differentiation, and function of TAMs; however, the discovery of selective CSF1R inhibitors devoid of type III kinase activity has proven to be challenging. We discovered a potent, highly selective, and orally bioavailable CSF1R inhibitor, IACS-9439 (1). Treatment with 1 led to a dose-dependent reduction in macrophages, promoted macrophage polarization toward the M1 phenotype, and led to tumor growth inhibition in MC38 and PANC02 syngeneic tumor models.
Methanol as hydrogen source: Transfer hydrogenation of aromatic aldehydes with a rhodacycle
Aboo, Ahmed H.,Bennett, Elliot L.,Deeprose, Mark,Robertson, Craig M.,Iggo, Jonathan A.,Xiao, Jianliang
supporting information, p. 11805 - 11808 (2018/11/10)
A cyclometalated rhodium complex has been shown to perform highly selective and efficient reduction of aldehydes, deriving the hydrogen from methanol. With methanol as both the solvent and hydrogen donor under mild conditions and an open atmosphere, a wide range of aromatic aldehydes were reduced to the corresponding alcohols, without affecting other functional groups.
NOXIOUS ARTHROPOD CONTROL COMPOSITION AND HETEROCYCLIC COMPOUND
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Paragraph 0754; 0755, (2013/04/13)
A noxious arthropod controlling composition comprising a heterocyclic compound represented by the formula (1) [wherein, A1 and A2 represent ═C(R6)—, nitrogen and so on, R1 represents a halogen and so on, R3