Indole is a compound of pyrrole and benzene in parallel, also known as benzopyrrole. There are two combinations of pyrrole and benzene, called indole and isoindole, respectively. Many derivatives of indole have physiological and pharmacological activities, and can synthesize vasodilators, antihistamines, antipyretic analgesics, etc. in medicine, so indole is also a very important heterocyclic compound.
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KRAS was once a notorious 'undruggable target' over the past few decades. Most cancers driven by KRAS mutations lack corresponding targeted drugs. Now, this dilemma is finally expected to be broken!
Revolution Medicines recently announced the publication of two peer-reviewed research papers in Nature. Two original papers highlight the discovery and translational implications of RMC-7977, a RAS(ON) multi-selective tri-complex inhibitor that exhibits unprecedented anti-tumor activity in preclinical models of RAS-mutant pancreatic ductal adenocarcinoma (PDAC). The first paper demonstrates RMC-7977 successfully targets signaling by both mutant and wild-type forms of RAS to drive potent and durable inhibition of RAS-mutated cancers. The second paper highlights the systematic evaluation of RMC-7977 in a wide range of preclinical models of PDAC. Oncogenic RAS proteins drive up to 30 percent of all human cancers, most notably non-small cell lung cancer (NSCLC), PDAC and colorectal cancer (CRC). RAS G12 mutations, such as G12D, G12V and G12C, predominate in human cancers. Approved KRAS-targeted cancer therapies target only one particular RAS mutation, KRAS G12C. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
Revolution Medicines announced preliminary positive data for its RAS(ON) G12D-selective covalent inhibitor RMC-9805 in previously treated pancreatic ductal adenocarcinoma (PDAC) patients. The analysis showed that the disease control rate of PDAC patients treated with RMC-9805 was as high as 80%. RMC-9805 is a potential ‘first-in-class’ oral RAS(ON) G12D-selective inhibitor, that is being evaluated in trials to examine its efficacy and safety in patients with solid tumors carrying KRAS G12D mutations when used as a single agent or in combination with the pan-RAS inhibitor RMC-6236. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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