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RMC-9805
RMC-9805 is an investigational drug that selectively targets the G12D mutation in KRAS dependent cancers. RMC-9805 functions as molecular glue that forms a non-covalent ligand-mediated protein-protein interaction between cyclophilin A and GTP-bound RAS. Subsequent covalent modification of the mutant Asp12 residue affords selectivity over wild-type RAS. RMC-9805 is currently in a phase 1/1b clinical trial for the treatment of KRAS G12D-mutant solid tumors. Preliminary data indicated that KRAS G12D–mutant PDAC patients dosed at 1200 mg daily or 600 mg twice daily achieved a 30% objective response rate (n = 12) and 80% disease control rate (n = 32). See also * ACBI3 * Adagrasib * MRTX1133 * Olomorasib * Sotorasib Sotorasib, sold under the brand names Lumakras and Lumykras, is an anti-cancer medication used to treat non-small-cell lung cancer. It targets a specific mutation, G12C, in the protein K-Ras encoded by gene KRAS which is responsible for vario ... ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
KRAS
''KRAS'' ( Kirsten rat sarcoma virus) is a gene that provides instructions for making a protein called K-Ras, a part of the RAS/MAPK pathway. The protein relays signals from outside the cell to the cell's nucleus. These signals instruct the cell to grow and divide ( proliferate) or to mature and take on specialized functions ( differentiate). It is called ''KRAS'' because it was first identified as a viral oncogene in the Kirsten RAt Sarcoma virus. The oncogene identified was derived from a cellular genome, so , when found in a cellular genome, is called a proto-oncogene. The K-Ras protein is a GTPase, a class of enzymes which convert the nucleotide guanosine triphosphate (GTP) into guanosine diphosphate (GDP). In this way the K-Ras protein acts like a switch that is turned on and off by the GTP and GDP molecules. To transmit signals, it must be turned on by attaching (binding) to a molecule of GTP. The K-Ras protein is turned off (inactivated) when it converts the GTP to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aziridines
220 px, chemotherapy.html" ;"title="Mitomycin C, an aziridine, is used as a chemotherapy">chemotherapeutic agent by virtue of its antitumour activity. In organic chemistry, aziridines are organic compounds containing the aziridine functional group (chemical structure ), a three-membered heterocycle with one amine () and two methylene bridges (). The parent compound is aziridine (or ethylene imine), with molecular formula . Several drugs feature aziridine rings, including zoldonrasib, thiotepa, mitomycin C, porfiromycin, and azinomycin B (carzinophilin). Structure The bond angles in aziridine are approximately 60°, considerably less than the normal hydrocarbon bond angle of 109.5°, which results in angle strain as in the comparable cyclopropane and ethylene oxide molecules. A banana bond model explains bonding in such compounds. Aziridine is less basic than acyclic aliphatic amines, with a pKa of 7.9 for the conjugate acid, due to increased s character of the nitrog ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ACBI3
ACBI3 is an experimental anticancer drug which is one of the first examples of a proteolysis targeting chimera or PROTAC. It is a bifunctional molecule with two halves joined by a linker; one half binds to a protein found in various forms of cancer cell called Kirsten rat sarcoma virus or KRAS, while the other half binds E3 ligase which triggers the cell's natural protein degradation mechanisms so that the entire complex is broken down. In early stage testing, it was able to target 13 of the 17 most common mutated forms of KRAS found in cancer cells, allowing selective targeting of a wide range of cancer types. While this particular molecule is still at an early developmental stage and may be unlikely to be approved as a medicine itself, it is an important proof of concept which is likely to lead to the development of a range of related PROTAC type anticancer drugs. See also * Adagrasib * K-Ras(G12C) inhibitor 6 * MRTX1133 * Olomorasib * RMC-9805 * Sotorasib Sotorasib ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MRTX1133
MRTX1133 is an investigational drug that targets the G12D mutation in KRAS dependent cancers. MRTX1133 was in a phase 1/2 clinical trial for the treatment of solid tumors, however the study was terminated in Q1 2025. MRTX1133 is considered to be harmful from direct skin or eye exposure other than transient irritation. It may cause irritation of the respiratory system if inhaled. See also * ACBI3 * Adagrasib * Olomorasib * RMC-9805 * Sotorasib Sotorasib, sold under the brand names Lumakras and Lumykras, is an anti-cancer medication used to treat non-small-cell lung cancer. It targets a specific mutation, G12C, in the protein K-Ras encoded by gene KRAS which is responsible for vario ... References {{antineoplastic-drug-stub Antineoplastic drugs Pyridopyrimidines Pyrrolizidines Fluoroarenes Ethynyl compounds Naphthols Aromatic ethers ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Olomorasib
Olomorasib (LY3537982) is an experimental anticancer drug which acts as an inhibitor of the G12C mutant form of Kirsten rat sarcoma virus (KRAS), an oncogene commonly present in several forms of cancer. It is in early stage clinical trials against lung and colorectal cancers and advanced solid tumors. See also * ACBI3 * Adagrasib * Divarasib * MRTX1133 * RMC-9805 * Sotorasib Sotorasib, sold under the brand names Lumakras and Lumykras, is an anti-cancer medication used to treat non-small-cell lung cancer. It targets a specific mutation, G12C, in the protein K-Ras encoded by gene KRAS which is responsible for vario ... References {{reflist Experimental cancer drugs Benzothiophenes Pyrazines Oxazocines Nitriles Fluoroarenes Chloroarenes Amines Carboxamides Cyclic ketones ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methoxy Compounds
In organic chemistry, a methoxy group is the functional group consisting of a methyl group bound to oxygen. This alkoxy group has the formula . On a benzene ring, the Hammett equation classifies a methoxy substituent at the ''para'' position as an electron-donating group, but as an electron-withdrawing group if at the ''meta'' position. At the ''ortho'' position, steric effects are likely to cause a significant alteration in the Hammett equation prediction, which otherwise follows the same trend as that of the ''para'' position. Occurrence The simplest of methoxy compounds are methanol and dimethyl ether. Other methoxy ethers include anisole and vanillin. Many metal alkoxides contain methoxy groups, such as tetramethyl orthosilicate and titanium methoxide. Esters with a methoxy group can be referred to as methyl esters, and the —COOCH3 substituent is called a methoxycarbonyl. Biosynthesis In nature, methoxy groups are found on nucleosides subjected to 2′-''O''-methyla ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclopentyl Compounds
Cyclopentane (also called C pentane) is a highly flammable alicyclic hydrocarbon with chemical formula C5H10 and CAS number 287-92-3, consisting of a ring of five carbon atoms each bonded with two hydrogen atoms above and below the plane. It is a colorless liquid with a petrol-like odor. Its freezing point is −94 °C and its boiling point is 49 °C. Cyclopentane is in the class of cycloalkanes, being alkanes that have one or more carbon rings. It is formed by cracking cyclohexane in the presence of alumina at a high temperature and pressure. It was first prepared in 1893 by the German chemist Johannes Wislicenus. Production, occurrence and use Cycloalkanes are formed by catalytic reforming. For example, when passed over a hot platinum surface, 2-methylbutane converts into cyclopentane. Cyclopentane is principally used as a blowing agent in the manufacture of polyurethane insulating foam, replacing ozone-depleting agents such as CFC-11 and HCFC-141b. [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lactones
Lactones are cyclic carboxylic esters. They are derived from the corresponding hydroxycarboxylic acids by esterification. They can be saturated or unsaturated. Lactones are formed by lactonization, the intramolecular esterification of the corresponding hydroxycarboxylic acids. Nomenclature Greek prefixes in alphabetical order indicate ring size. Lactones are usually named according to the precursor acid molecule (''aceto'' = 2 carbon atoms, ''propio'' = 3, ''butyro'' = 4, ''valero'' = 5, ''capro'' = 6, etc.), with a ''-lactone'' suffix and a Greek letter prefix that specifies the number of carbon atoms in the heterocycle — that is, the distance between the relevant -OH and the -COOH groups along said backbone. The first carbon atom after the carbon in the -COOH group on the parent compound is labelled α, the second will be labeled β, and so forth. Therefore, the prefixes also indicate the size of the lactone ring: α-lactone = 3-membered ring, β-lactone = 4-membered, γ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Morpholines
Morpholine is an organic chemical compound having the chemical formula O( C H2CH2)2 NH. This heterocycle features both amine and ether functional groups. Because of the amine, morpholine is a base; its conjugate acid is called morpholinium. For example, treating morpholine with hydrochloric acid generates the salt morpholinium chloride. It is a colorless liquid with a weak, ammonia- or fish-like odor. The naming of morpholine is attributed to Ludwig Knorr, who incorrectly believed it to be part of the structure of morphine. Production Morpholine is often produced industrially by the dehydration of diethanolamine with concentrated sulfuric acid. Alternatively, it can be made from bis(2-chloroethyl)ether in a reaction with ammonia, by which also ammonium chloride is formed. Morpholine is also produced industrially from diethylene glycol and ammonia, under high temperature and pressure, in the presence of hydrogen and a suitable catalyst. Uses Industrial applications Morpholin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indoles
Indole is an organic compound with the formula . Indole is classified as an aromatic Heterocyclic compound, heterocycle. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered pyrrole ring. Indoles are derivatives of indole where one or more of the hydrogen atoms have been replaced by substituent groups. Indoles are widely distributed in nature, most notably as amino acid tryptophan and neurotransmitter serotonin. General properties and occurrence Indole is a solid at room temperature. It occurs naturally in human feces and has an intense fecal odor. At very low concentrations, however, it has a flowery smell, and is a constituent of many perfumes. It also occurs in coal tar. It has been identified in cannabis. It is the main volatile compound in stinky tofu. When indole is a substituent on a larger molecule, it is called an ''indolyl group'' by systematic nomenclature. Indole undergoes electrophilic substitution, mainly at position ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
