It’s only fair to share… Atirmociclib CAS 2380321-51-5 MF C22H27ClFN5O3, 463.9 g/mol (3S,4R)-4-[[5-chloro-4-[7-fluoro-2-(2-hydroxypropan-2-yl)-3-propan-2-ylbenzimidazol-5-yl]pyrimidin-2-yl]amino]oxan-3-ol (3S,4R)-4-({5-chloro-4-[4-fluoro-2-(2-hydroxypropan-2-yl)-1-(propan2-yl)-1H-1,3-benzimidazol-6-yl]pyrimidin-2-yl}amino)oxan-3-ol 1,5-anhydro-3-({5-chloro-4-[4-fluoro-2-(2-hydroxpropan-2-yl)-1-(propan-2-yl)-1H-benzimidazol-6-yl]pyrimidin-2-yl}amino)-2,3-dideoxy-D-threo-pentitol D-threo-Pentitol, 1,5-anhydro-3-[[5-chloro-4-[4-fluoro-2-(1-hydroxy-1-methylethyl)-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinyl]amino]-2,3-dideoxy-cyclin-dependent kinase (CDK) inhibitor, antineoplastic, PF 07220060, S743GOJ5LJ, CDK4/6-IN-6 Atirmociclib is an orally bioavailable inhibitor of cyclin-dependent kinase 4 (CDK4), with potential antineoplastic activity. Upon administration, atirmociclib selectively inhibits CDK4, which inhibits the phosphorylation of retinoblastoma protein (Rb) early in …
Tag «Antineoplastic»
Asaretoclax
It’s only fair to share… Asaretoclax CAS 2363074-01-3 MF C47H57F2N7O7S, MW 902.1 g/mol 4-[4-[[2-[3-(difluoromethyl)-1-bicyclo[1.1.1]pentanyl]-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[4-[(4-hydroxy-4-methylcyclohexyl)methylamino]-3-nitrophenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((2-(3-(difluoromethyl)bicyclo[1.1.1]pentan-1-yl)-4,4-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)-N-((4-((((1r,4r)-4-hydroxy-4-methylcyclohexyl)methyl)amino)-3-nitrophenyl)sulfonyl)benzamide B-cell lymphoma 2 (Bcl-2) inhibitor, antineoplastic, GY6FD5FXA3, HY 159817, ABT 263 Asaretoclax is an orally bioavailable inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (Bcl-2), with potential pro-apoptotic and antineoplastic activities. Upon oral administration, asaretoclax targets, binds to and inhibits the …
Zomiradomide
It’s only fair to share… Zomiradomide CAS 2655656-99-6 MF C45H48F3N7O6S MW871.97 antineoplastic, IRAK degrader-1, AQ5UXV5646 Zomiradomide is an orally active PROTAC degrader for IRAK4 (DC50=6 nM), thereby inhibiting the NF-κB signaling pathway. Zomiradomide acts also as a molecular glue, recruiting Ikaros and Aiolos, and mediating their degradation (DC50 for Ikaros is 1 nM), thereby activating the type I IFN signaling pathway. Zomiradomide …
Zemirciclib
It’s only fair to share… Zemirciclib CAS 2057509-72-3 MF C22H28ClN5O2, 429.9 g/mol (1S,3R)-3-acetamido-N-[5-chloro-4-(5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-yl]cyclohexane-1-carboxamide (1S,3R)-3-acetamido-N-[5-chloro-4-(5,5-dimethyl-4,6-dihydropyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-yl]cyclohexane-1-carboxamide (1S,3R)-3-acetamido-N-(5-chloro-4-(5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-yl)cyclohexanecarboxamide cyclin-dependent kinase inhibitor, antineoplastic, AZD 4573, UNII-E5XSP3X68B Zemirciclib is a selective, short-acting inhibitor of the serine/threonine cyclin-dependent kinase 9 (CDK9), the catalytic subunit of the RNA polymerase II (RNA Pol II) elongation factor positive transcription elongation factor b (PTEF-b; PTEFb), with potential antineoplastic …
Zelenirstat
It’s only fair to share… Zelenirstat CAS 1215011-08-7 MF C24H30Cl2N6O2S, 537.5 g/mol 2,6-dichloro-N-[1,5-dimethyl-3-(2-methylpropyl)-1Hpyrazol-4-yl]-4-[2-(piperazin-1-yl)pyridin-4-yl]benzene-1-sulfonamideN-myristoyltransferase inhibitor, antineoplastic, PCLX 001, DDD86481, CCI 002, DDD 86481 Zelenirstat (PCLX-001) is an investigational, oral small-molecule drug that inhibits N-myristoyltransferases (NMTs), enzymes crucial for adding fatty acids to proteins, a process vital for cell signaling and membrane attachment. Developed by Pacylex Pharmaceuticals, it’s being tested …
Zamzetoclax
It’s only fair to share… Zamzetoclax CAS 2388470-64-0 MF C38H46ClN5O6S MW736.32 N-[(3′R,4S,6′R,7′S,8′E,11′S)-7-chloro-7′-methoxy-11′-methyl-13′,15′-dioxospiro[2,3-dihydro-1H-naphthalene-4,22′-20-oxa-13λ6-thia-1,14-diazatetracyclo[14.7.2.03,6.019,24]pentacosa-8,13,16(25),17,19(24)-pentaene]-13′-yl]-3-methoxy-1-methylpyrazole-4-carboxamide B-cell lymphoma 2 (Bcl-2) inhibitor, antineoplastic, RRS8GZU2UN Zamzetoclax (compound 1) is a potential Mcl-1 inhibitor. REFDiscovery of an Oral, Beyond-Rule-of-Five Mcl-1 Protein–Protein Interaction Modulator with the Potential of Treating Hematological Malignancies Publication Name: Journal of Medicinal Chemistry Publication Date: 2023-04-28 PMID: 37114951 DOI: 10.1021/acs.jmedchem.2c01953 SYN WO 2019/222112 https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2019222112&_cid=P12-MJ7Z15-98773-1 Example …
Vilzemetkib
It’s only fair to share… Vilzemetkib CAS 1363402-44-1 MF C36H36F2N4O5 MW 642.7 g/mol 1-N‘-[4-[7-[[1-(cyclopentylamino)cyclopropyl]methoxy]-6-methoxyquinolin-4-yl]oxy-3-fluorophenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide hepatocyte growth factor receptor inhibitor, antineoplastic, AL 2846, FJ4Y6XP24Y Vilzemetkib (also known as AL2846) is an investigational, orally active small-molecule drug that acts as a potent inhibitor of the c-Met receptor tyrosine kinase, a protein often overexpressed in cancers, aiming to block tumor growth, …
Tigozertinib
It’s only fair to share… Tigozertinib CAS 2660250-10-0 MF C28H37FN6O3S MW 556.7 3-Isoquinolinamine, N-[2-[(3S,4R)-3-fluoro-4-methoxy-1-piperidinyl]-4-pyrimidinyl]-5-(1-methylethyl)-8-[(2R,3S)-2-methyl-3- [(methylsulfonyl)methyl]-1-azetidinyl]- N-{2-[(3S,4R)-3-fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl}-8-{(2R,3S)-3-[(methanesulfonyl)methyl]-2-methylazetidin-1-yl}-5-(propan-2-yl)isoquinolin-3-amine N-[2-[(3S,4R)-3-fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl]-8-[(2R,3S)-2-methyl-3-(methylsulfonylmethyl)azetidin-1-yl]-5-propan-2-ylisoquinolin-3-amine N-(2-((3S,4R)-3-fluoro-4-methoxypiperidin-l-yl)pyrimidin-4-yl)-5-isopropyl-8-(3-(methylsulfonylmethyl)azetidin-l-yl)isoquinolin-3-amine epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, antineoplastic, PA4PTH5HL9, BLU 945 Tigozertinib (BLU-945) is currently under investigation in clinical trial NCT04862780 (Phase 1/2 Study Targeting EGFR Resistance Mechanisms in NSCLC) for the treatment of NSCLC. Tigozertinib …
Tambiciclib
It’s only fair to share… Tambiciclib CAS 2247481-08-7 MF C25H35ClN6O2S, 519.10 4-[[[4-[5-chloro-2-[[4-[[(2R)-1-methoxypropan-2-yl]amino]cyclohexyl]amino]-4-pyridinyl]-1,3-thiazol-2-yl]amino]methyl]oxane-4-carbonitrile 2H-PYRAN-4-CARBONITRILE, 4-(((4-(5-CHLORO-2-((TRANS-4-(((1R)-2-METHOXY-1-METHYLETHYL)AMINO)CYCLOHEXYL)AMINO)-4-PYRIDINYL)-2-THIAZOLYL)AMINO)METHYL)TETRAHYDRO- cyclin-dependent kinase inhibitor, antineoplastic, GFH 009, JSH 009, XDZ7VK8CXC, Orphan Drug , Acute myeloid leukaemia, Peripheral T-cell lymphoma Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent …
Talorasib
It’s only fair to share… Talorasib CAS 2648584-48-7 MFC32H34ClFN6O3 MW605.10 [(2S)-4-[(7S)-7-(8-chloronaphthalen-1-yl)-2-{[(2S)-1-methylpyrrolidin-2-yl]methoxy}-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-4-yl]-1-(2-fluoroprop-2-enoyl)piperazin-2-yl]acetonitrileKirsten rat sarcoma viral oncogene homologue (KRAS)inhibitor, antineoplastic, 727W6T7DPK SYN CN115385923 https://patentscope.wipo.int/search/en/detail.jsf?docId=CN380619664&_cid=P20-MJ0TAW-52678-1 Preparation Example 1: Synthesis of the compound shown in formula (I) (1) Synthesis of Compound 1 Synthetic route of compound 1: Synthesis of compound 1-j 1-Bromo-8-chloronaphthalene (500 mg, 2.07 mmol) was dissolved in …